Search Result
Results for "
opioid antagonist
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
15
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-17417
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Opioid Receptor
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Neurological Disease
Cancer
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Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias .
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- HY-101718
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- HY-17417A
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Opioid Receptor
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Neurological Disease
Cancer
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Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias .
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- HY-19627A
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S-297995 tosylate
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Opioid Receptor
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Neurological Disease
Metabolic Disease
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Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
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- HY-76711
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Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight .
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- HY-107744
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- HY-A0118A
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NKTR-118 oxalate; AZ-13337019 oxalate
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Opioid Receptor
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Metabolic Disease
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Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol oxalate inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol oxalate is applicable to research related to opioid-induced constipation .
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- HY-13243
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ADL 8-2698; LY 246736
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Opioid Receptor
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Neurological Disease
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Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
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- HY-10487
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- HY-13274
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- HY-100903
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nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
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Opioid Receptor
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Neurological Disease
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Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
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- HY-117040
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Norbinaltorphimine; NorBNI
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Opioid Receptor
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Neurological Disease
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nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .
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- HY-101302
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Opioid Receptor
TRP Channel
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Inflammation/Immunology
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Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows Ki values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer .
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- HY-123689
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ALKS-33; RDC-0313
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Opioid Receptor
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Neurological Disease
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Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals .
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- HY-101376
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(+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride
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Opioid Receptor
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Neurological Disease
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(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease .
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- HY-107749
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- HY-101011
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- HY-107748
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5'-GNTI hydrochloride
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Opioid Receptor
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Neurological Disease
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5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor .
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- HY-100122
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- HY-108229
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6β-Hydroxynaltrexone
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Drug Metabolite
Opioid Receptor
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Neurological Disease
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6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
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- HY-19627
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S-297995
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Opioid Receptor
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Neurological Disease
Metabolic Disease
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Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
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- HY-137279
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Opioid Receptor
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Inflammation/Immunology
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Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier .
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- HY-136208
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Opioid Receptor
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Neurological Disease
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TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
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- HY-W013154
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Amino Acid Derivatives
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Others
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Fmoc-Tic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as the biotinylated derivative of the opioid receptor antagonist TIPP .
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- HY-D1387
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Fluorescent Dye
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Neurological Disease
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Naloxone fluorescein acetate is the fluorescent-derivative of Naloxone. Naloxone is an opioid antagonist. Naloxone is the antidote for reversing the effects of an opioid overdose .
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- HY-76711R
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Reference Standards
Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Naltrexone (Standard) is the analytical standard of Naltrexone (HY-76711). This product is intended for research and analytical applications. Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
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- HY-174422
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Opioid Receptor
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Others
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Opioid receptor antagonist 2 (Compound 9) is a potent opioid receptor antagonist. Opioid receptor antagonist 2 can reverse ventilatory depression and vocal cord closure induced by fentanyl analogs in mice. Opioid receptor antagonist 2 is promising for research of acute poisoning such as respiratory depression caused by overdose of opioids .
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- HY-101307
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7-Benzylidenenaltrexone maleate
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Opioid Receptor
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Neurological Disease
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BNTX (7-Benzylidenenaltrexone) maleate is a δ1-opioid receptor antagonist with the Kis of 0.1, 10.8, 13.3, and 58.6 nM for δ1, δ2-, μ-, and κ-opioid receptor, respectively. BNTX maleate shows antinociceptive activity .
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- HY-17417R
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Reference Standards
Opioid Receptor
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Neurological Disease
Cancer
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Naloxone (hydrochloride) (Standard) is the analytical standard of Naloxone (hydrochloride). This product is intended for research and analytical applications. Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias .
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- HY-107750A
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Opioid Receptor
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Neurological Disease
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Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect .
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- HY-76657A
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ADL 8-2698 dihydrate; LY 246736 dihydrate
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Opioid Receptor
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Neurological Disease
Cancer
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Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
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- HY-16979
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Opioid Receptor
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Neurological Disease
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RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects .
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- HY-107121
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LY 2196044
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Opioid Receptor
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Neurological Disease
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Ondelopran (LY 2196044) is a non-selective opioid receptor antagonist. Ondelopran inhibits the release of dopamine in the nucleus accumbens induced by alcohol, reduces the rewarding effect of alcohol consumption, and lowers the craving. Ondelopran can be used for alcohol use disorder (AUD) .
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- HY-144609
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .
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- HY-107743
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NalBzoH
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Opioid Receptor
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Neurological Disease
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Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect .
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- HY-155320
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC50 of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder .
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- HY-10486
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- HY-144607
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
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- HY-144606
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .
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- HY-156614
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- HY-101233
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- HY-169867
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7-Benzylidenenaltrexone
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Opioid Receptor
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Neurological Disease
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BNTX (7-Benzylidenenaltrexone) is a highly selective δ1 opioid receptor antagonist. BNTX selectively antagonizes the antinociceptive activity mediated by spinal δ1 opioid receptors, and does not alter the antinociceptive effects mediated by δ2, μ or κ opioid receptors at selective doses .
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- HY-114072A
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- HY-178235
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Opioid Receptor
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Neurological Disease
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MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia .
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- HY-19902
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Opioid Receptor
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Neurological Disease
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GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and agents .
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- HY-N12180A
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- HY-B1485
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Opioid Receptor
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Neurological Disease
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Nalmefene hydrochloride is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence .
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- HY-163895
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Fluorescent Dye
Opioid Receptor
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Neurological Disease
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δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception .
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- HY-175661
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Opioid Receptor
Beta-secretase
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Neurological Disease
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SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease .
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- HY-170654
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Opioid Receptor
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Neurological Disease
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Opioid receptor antagonist 1 (Compound 10) is an Orvinol (HY-D0168)-based opioid receptor antagonist. Opioid receptor antagonist 1 has antagonistic activity to the analgesic properties of Morphine .
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- HY-123689S1
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ALKS-33-d5; RDC-0313-d5
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Isotope-Labeled Compounds
Opioid Receptor
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Neurological Disease
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Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
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- HY-162669
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 8 (368) is a μ-opioid receptor antagonist. Mu opioid receptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi .
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- HY-144608
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .
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- HY-144610
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD) .
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- HY-A0118
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NKTR-118; AZ-13337019
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Opioid Receptor
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Neurological Disease
Cancer
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Naloxegol (NKTR-118; AZ-13337019) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol is applicable to research related to opioid-induced constipation .
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- HY-17417AS
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Opioid Receptor
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Others
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Naloxone D5 is deuterium labeled Naloxone. Naloxone is a a potent opioid receptor antagonist.
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- HY-135698
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M-CAM
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Opioid Receptor
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Neurological Disease
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Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction .
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- HY-106732
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Opioid Receptor
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Neurological Disease
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AT-076 is an opioid pan antagonist at nociception, kappa, mu, and delta opioid receptors, with Ki values of 1.75 nM (NOP), 1.67 nM (MOP), 1.14 nM (KOP) and 19.6 nM (DOP), respectively .
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- HY-133717
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Opioid Receptor
TRP Channel
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Cancer
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Naltriben is a selective δ2-opioid receptor antagonist and TRPM7 activator. Naltriben enhances glioblastoma cell migration and invasion. Naltriben can be used in research into neurological diseases and cancer .
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- HY-106601A
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LY-150720 hydrochloride
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Opioid Receptor
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Neurological Disease
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Picenadol (LY-150720) hydrochloride is an opioid mixed agonist-antagonist analgesic. Picenadol hydrochloride is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol hydrochloride has anticholinergic activity .
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- HY-76657
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ADL 8-2698 monohydrate; LY 246736 monohydrate
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Opioid Receptor
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Neurological Disease
Cancer
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Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus .
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- HY-101317A
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SB-205607
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Opioid Receptor
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Metabolic Disease
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TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
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- HY-120927A
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Opioid Receptor
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Neurological Disease
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Alvimopan metabolite hydrochloride is a peripherally restricted Opioid Receptor antagonist that inhibits the amplitude of electrically evoked contractions and spontaneous mechanical activity in guinea pig ileum .
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- HY-W001874
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3-Hydrazinylpropanenitrile
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Drug Intermediate
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Others
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2-Cyanoethylhydrazine (3-Hydrazinylpropanenitrile) is a drug synthesis intermediate that can be used to synthesize an antagonist of opioid receptor-like 1 (ORL1) .
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- HY-101223
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Opioid Receptor
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Neurological Disease
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DIPPA hydrochloride is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA hydrochloride can be used for the research of anxiety and antidepressant .
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- HY-P10395
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- HY-120277
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- HY-179282
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a Ki of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD) .
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- HY-176505
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Opioid Receptor
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Neurological Disease
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NOP antagonist 1 (Compound (-)-31) is a nociceptin opioid peptide (NOP) antagonist with a Kb of 8.65 nM. NOP antagonist 1 can be used for neuropsychiatric disorders research .
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- HY-17417AR
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Opioid Receptor
Reference Standards
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Neurological Disease
Cancer
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Naloxone (Standard) is the analytical standard of Naloxone. This product is intended for research and analytical applications. Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias .
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- HY-107744R
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- HY-147560
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Sigma Receptor
Opioid Receptor
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Neurological Disease
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σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain .
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- HY-123689A
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ALKS-33 hydrochloride; RDC-0313 hydrochloride
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Opioid Receptor
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Neurological Disease
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Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals .
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- HY-123689S
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ALKS-33-d4; RDC-0313-d4
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Isotope-Labeled Compounds
Opioid Receptor
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Neurological Disease
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Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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- HY-123689R
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ALKS-33 (Standard); RDC-0313 (Standard)
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Opioid Receptor
Reference Standards
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Neurological Disease
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Samidorphan (Standard) is the analytical standard of Samidorphan. This product is intended for research and analytical applications. Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals.
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- HY-120927
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Opioid Receptor
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Neurological Disease
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Alvimopan metabolite is a μ opioid receptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioid receptor antagonist during research and development .
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- HY-107748A
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5'-GNTI TFA
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Endogenous Metabolite
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Neurological Disease
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5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency .
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- HY-112263
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- HY-169822
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- HY-177790
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin receptor antagonist 7 (Compound 34) is an antagonist of the orexin receptor (OX1R), with a Ki value of 4.05 nM. Orexin receptor antagonist 7 shows no detectable activity towards OX2R and has very low affinities for the three opioid receptors (μ, δ, κ) (Ki > 1,000 nM). Orexin receptor antagonist 7 can be used for research on opioid addiction .
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- HY-A0118AS
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Isotope-Labeled Compounds
Opioid Receptor
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Neurological Disease
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Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
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- HY-P2669
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- HY-A0118S
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NKTR-118-13C,d3; AZ-13337019-13C,d3
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Isotope-Labeled Compounds
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Neurological Disease
Cancer
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Naloxegol- 13C,d3 (NKTR-118- 13C,d3) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
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- HY-A0118S1
-
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NKTR-118-13C,d2; AZ-13337019-13C,d2
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Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
Cancer
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Naloxegol- 13C,d2 (NKTR-118- 13C,d2) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
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- HY-158236
-
-
- HY-129422
-
-
- HY-123142
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-
- HY-117881
-
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Opioid Receptor
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Neurological Disease
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CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
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- HY-118615
-
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Opioid Receptor
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Neurological Disease
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LY2048978 is a non-selective opioid receptor antagonist with Ki of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder .
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-
- HY-P10177
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Opioid Receptor
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Neurological Disease
|
|
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
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- HY-P10175
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Opioid Receptor
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Neurological Disease
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Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
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- HY-106601
-
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LY-150720
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Opioid Receptor
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Neurological Disease
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Picenadol (LY-150720) is an opioid mixed agonist-antagonist analgesic. Picenadol is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol has anticholinergic activity .
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- HY-167946
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Opioid Receptor
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Others
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CP-866087 is a new, highly effective, and selective antagonist of the mu-opioid receptor designed for exploring female sexual dysfunction.
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- HY-101199
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Opioid Receptor
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Neurological Disease
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N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function .
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- HY-N2304A
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Opioid Receptor
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Inflammation/Immunology
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Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract .
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- HY-107750
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- HY-13243R
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ADL 8-2698 (Standard); LY 246736 (Standard)
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Opioid Receptor
Reference Standards
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Neurological Disease
Cancer
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Alvimopan (Standard) is the analytical standard of Alvimopan. This product is intended for research and analytical applications. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
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-
- HY-16765A
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TD-1211 sulfate
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Opioid Receptor
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Neurological Disease
|
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Axelopran sulfate is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
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- HY-181605
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Opioid Receptor
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Neurological Disease
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MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder .
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-
- HY-100903R
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nor-Binaltorphimine dihydrochloride (Standard); nor-BNI dihydrochloride (Standard)
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Opioid Receptor
Reference Standards
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Neurological Disease
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Norbinaltorphimine dihydrochloride (Standard) is the analytical standard of Norbinaltorphimine dihydrochloride (HY-100903). This product is intended for research and analytical applications. Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
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- HY-P10394
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- HY-101230
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Opioid Receptor
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Neurological Disease
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ICI 174864 is a selective and brain-penetrant δ-opioid receptor antagonist with Ke values of 22.0 nM to 30.6 nM at δ-opioid receptor in mouse vas deferens. ICI 174864 selectively blocks biological effects mediated by the δ-opioid receptor agonist DPDPE (HY-P1334) after central administration. ICI 174864 reverses hypotension in rats with endotoxic shock and inhibits acetic acid-induced writhing in mice. ICI 174864 can be used for the research of opioid receptor subtypes, endotoxic hypotension and analgesic pathways .
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- HY-P1335
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CTAP
2 Publications Verification
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Opioid Receptor
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Neurological Disease
|
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CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-76711S
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Isotope-Labeled Compounds
Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Naltrexone-d4 is deuterium labeled Naltrexone (HY-76711). Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
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- HY-13243S1
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ADL 8-2698-d7; LY 246736-d7
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Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
Cancer
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Alvimopan-d7 (ADL 8-2698-d7) is deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
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- HY-13274A
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- HY-P2052
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Opioid Receptor
Neurokinin Receptor
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Others
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AWL 60 is a compound with SP antagonist and weak opioid agonist properties, which can antagonize SP-agonists in vitro and attenuate the decrease in blood pressure caused by SP-agonists in vivo.
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- HY-123582
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Opioid Receptor
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Neurological Disease
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CP-866,087 is a novel, potent and selective μ-opioid receptor antagonist with activity to inhibit opioid effects. CP-866,087 has shown promising preclinical efficacy data in disease models associated with alcohol consumption. CP-866,087 has also been used to study female sexual dysfunction .
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- HY-P5892
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Opioid Receptor
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Neurological Disease
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β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioid receptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .
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-
- HY-N12180
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-
- HY-16765
-
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TD-1211
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Opioid Receptor
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Neurological Disease
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Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
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- HY-P1335A
-
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Opioid Receptor
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Neurological Disease
|
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CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-A0115R
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HOE 498 diacid (Standard); Ramipril diacid (Standard)
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Drug Metabolite
Reference Standards
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
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Cardiovascular Disease
|
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Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
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-
- HY-76657AR
-
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ADL 8-2698 dihydrate (Standard); LY 246736 dihydrate (Standard)
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Reference Standards
Opioid Receptor
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Neurological Disease
Cancer
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|
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
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- HY-107745
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-
- HY-135230
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FP3FBZ
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Opioid Receptor
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Neurological Disease
|
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LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ~1 nM. LY2444296 exhibits anti-anxiety like effects .
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- HY-115066
-
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Opioid Receptor
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Neurological Disease
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GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents .
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- HY-115066A
-
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Opioid Receptor
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Neurological Disease
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GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents .
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- HY-114072
-
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Opioid Receptor
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Neurological Disease
|
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J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors .
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- HY-107749R
-
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Reference Standards
Opioid Receptor
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Neurological Disease
|
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ML 190 (Standard) is the analytical standard of ML 190 (HY-107749). This product is intended for research and analytical applications. ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively .
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- HY-176063
-
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TRP Channel
Opioid Receptor
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Neurological Disease
|
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TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .
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- HY-A0142
-
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Adrenergic Receptor
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Endocrinology
|
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Dapiprazole is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole suppresses the opioid withdrawal symptoms. Dapiprazole is also used as eye drops for reversing mydriasis .
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- HY-A0142A
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Adrenergic Receptor
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Endocrinology
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Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis .
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- HY-136786
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-
- HY-116181
-
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Dopamine Receptor
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Neurological Disease
|
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YQA14 is a high affinity dopamine D3 receptor antagonist. YQA14 is anti-opioid addiction agent. YQA14 inhibits Morphine/Cocaine-induced conditioned place preference (CPP) in animals .
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- HY-149387
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Dopamine Receptor
Opioid Receptor
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Inflammation/Immunology
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D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
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- HY-149386
-
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Dopamine Receptor
Opioid Receptor
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Inflammation/Immunology
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D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
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- HY-116649
-
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AM4113
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Cannabinoid Receptor
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Neurological Disease
Metabolic Disease
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CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction .
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-
- HY-108229S
-
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6β-Hydroxynaltrexone-d3
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Isotope-Labeled Compounds
Opioid Receptor
Drug Metabolite
|
Neurological Disease
|
|
6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
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- HY-15708
-
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Opioid Receptor
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Neurological Disease
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LY2795050 is a short-acting selective κκ-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction .
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-
- HY-101718R
-
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CERC-501 (Standard); LY-2456302 (Standard)
|
Reference Standards
Opioid Receptor
|
Neurological Disease
|
|
Aticaprant (Standard) (CERC-501 (Standard)) is the analytical standard of Aticaprant (HY-101718). This product is intended for research and analytical applications. Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
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-
- HY-168366
-
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Opioid Receptor
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Neurological Disease
|
|
R-6890 is a Brorphine-related opioid receptor antagonist that exhibits differential binding activities toward rat opioid receptors (IC50=4.6 nM (0.05 M Tris; pH 7.4) and 170 nM (0.05 M Tris+0.1 M NaCl)). R-6890 displaces bound labeled opioids from receptors, and its binding affinity is affected by environmental factors, decreasing in the presence of NaCl. R-6890 crosses the blood-brain barrier (BBB) and exerts analgesic effects in the warm water-induced tail-flick reflex model of male Wistar rats .
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- HY-11052A
-
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Opioid Receptor
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Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
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-
- HY-170437
-
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Opioid Receptor
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Neurological Disease
|
|
MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Kis of 0.25, 41.1, 1.30 nM, respectively[1]
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-
- HY-W739948
-
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Isotope-Labeled Compounds
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Others
|
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Naltrexone-d3 is a deuterated labeled Naltrexone (HY-76711) . Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system .
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-
- HY-10487R
-
|
|
Reference Standards
Opioid Receptor
|
Neurological Disease
|
|
JDTic dihydrochloride (Standard) is the analytical standard of JDTic dihydrochloride (HY-10487). This product is intended for research and analytical applications. JDTic dihydrochloride is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
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- HY-145404
-
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Opioid Receptor
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Metabolic Disease
|
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Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .
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- HY-122561
-
|
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Opioid Receptor
|
Neurological Disease
|
|
MK-1925 is an orally active, CNS-penetrant ORL1 receptor antagonist with an IC50 of 8.2 nM. MK-1925 selectively inhibits the ORL1 receptor and shows no significant activity against other opioid receptors or the hERG potassium channel .
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-
- HY-P1329
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
-
- HY-124754
-
|
BTRX-335140; CYM-53093
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
|
-
- HY-P2429
-
|
|
Opioid Receptor
|
Others
|
|
N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a compound that can antagonize the δ-opioid receptor and the action of [D-Pen2,D-Pen ] enkephalin in vivo. Its antagonistic effect can be verified by specific behavioral experiments.
|
-
- HY-174307
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction) .
|
-
- HY-B0188A
-
|
Org GB 94
|
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-B0188
-
|
Mianserine
|
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
|
|
Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-163065
-
|
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
|
-
- HY-B0193
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Prazosin is an α-adrenergic receptor antagonist. Prazosin can reduce inflammation, relieve anxiety, alleviate panic, prevent memory decline, and modulate the pain-relieving effects of opioids. Prazosin can be used in the study of hypertension and Alzheimer’s disease .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-172149
-
|
5'-NTII
|
Opioid Receptor
|
Neurological Disease
|
|
Naltrindole 5′-isothiocyanate (5'-NTII) is a non-selective delta opioid receptor antagonist that can antagonize the analgesic effects induced by DSLET (HY-P1332) without affecting the analgesic effects induced by DPDPE (HY-P1334) .
|
-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
|
-
- HY-159923
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .
|
-
- HY-118949
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity .
|
-
- HY-A0142AR
-
|
|
Adrenergic Receptor
Reference Standards
|
Endocrinology
|
|
Dapiprazole (hydrochloride) (Standard) is the analytical standard of Dapiprazole (hydrochloride). This product is intended for research and analytical applications. Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis .
|
-
- HY-B0188AS
-
|
Org GB 94-d3
|
Isotope-Labeled Compounds
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-10672
-
|
|
Urotensin Receptor
Cytochrome P450
Sodium Channel
Opioid Receptor
|
Cardiovascular Disease
|
|
Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
|
-
- HY-12392A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Iprindole hydrochloride, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole hydrochloride shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole hydrochloride induces lamellar body formation but devoid of lamellar bodies. Iprindole hydrochloride can be used for the research of depression .
|
-
- HY-P3839
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
|
-
- HY-124583
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PF-4363467, a dopamine D3/D2 receptor antagonist, attenuates opioid drug-seeking behavior without
concomitant D2 side effects. PF-4363467 exhibits Ki values of 3.1 nM and 692 nM for D3R and D2R .
|
-
- HY-12392
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Iprindole, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole induces lamellar body formation but devoid of lamellar bodies. Iprindole can be used for the research of depression .
|
-
- HY-176710A
-
|
|
Drug Isomer
|
Others
|
|
(R)-PAD-PF2 is an isomer of PAD-PF2 (HY-176710). PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM).
|
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-134189
-
|
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
|
-
- HY-109067A
-
|
VVZ-149 hydrochloride
|
GlyT
5-HT Receptor
P2X Receptor
|
Neurological Disease
|
|
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
|
-
- HY-109067
-
|
VVZ-149
|
GlyT
5-HT Receptor
P2X Receptor
|
Neurological Disease
|
|
Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .
|
-
- HY-B0188AR
-
|
Org GB 94 (Standard)
|
Reference Standards
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-B0188S
-
|
Mianserine-d3
|
Histamine Receptor
Isotope-Labeled Compounds
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
|
|
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
- HY-134189A
-
|
|
Sigma Receptor
Opioid Receptor
|
Neurological Disease
|
|
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
|
-
- HY-155706
-
|
|
Opioid Receptor
Dopamine Receptor
|
Inflammation/Immunology
|
|
MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism .
|
-
- HY-W754114
-
-
- HY-125790
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Cyclazocine is a μ, δ, and κ opioid receptor modulator with Ki values of 0.32, 1.1, and 0.18 nM, respectively. Cyclazocine exhibits "mixed" pharmacological activities, acting as a μ-partial antagonist, κ-agonist, and low-affinity δ ligand. Cyclazocine shows antinociceptive activity in mice. Cyclazocine can be used in studies on psychoactive substance addiction .
|
-
- HY-122286
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease .
|
-
- HY-11056
-
|
|
Dopamine Receptor
|
Neurological Disease
|
PF-04363467 is a highly preferring D3R antagonist. PF-04363467 produces dose-dependent changes in the EEG profile of freely moving rats. PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-04363467 can be used for the study of addiction, cognitive and mental illness .
|
-
- HY-129668
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Bremazocine is a potent opioid kappa receptor agonist with analgesic activity. Bremazocine induces peripheral analgesia by releasing endogenous norepinephrine. The analgesic effect of bremazocine is associated with interaction with adenosine receptors. Bremazocine produces a dose-dependent peripheral analgesia after topical application. The effect of bremazocine is affected by nonselective α(2) adrenaline receptor antagonists, suggesting that it acts through a norepinephrine pathway .
|
-
- HY-12392R
-
|
|
Reference Standards
Opioid Receptor
|
Neurological Disease
|
|
Iprindole (Standard) is the analytical standard of Iprindole. This product is intended for research and analytical applications. Iprindole, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole induces lamellar body formation but devoid of lamellar bodies. Iprindole hydrochloride can be used for the research of depression .
|
-
- HY-106605
-
|
LY 120363
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .
|
-
- HY-119733
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
|
-
- HY-101318
-
|
β-FNA hydrochloride
|
Opioid Receptor
p38 MAPK
STAT
NF-κB
NO Synthase
Toll-like Receptor (TLR)
|
Cardiovascular Disease
Neurological Disease
|
|
β-Funaltrexamine (β-FNA) hydrochloride is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine hydrochloride inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine hydrochloride inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine hydrochloride is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases .
|
-
- HY-160938
-
|
β-FNA
|
Opioid Receptor
STAT
NF-κB
Toll-like Receptor (TLR)
NO Synthase
p38 MAPK
|
Cardiovascular Disease
Neurological Disease
|
|
β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases .
|
-
- HY-109067AR
-
|
VVZ-149 hydrochloride (Standard)
|
Reference Standards
GlyT
5-HT Receptor
P2X Receptor
|
Neurological Disease
|
|
Opiranserin hydrochloride (Standard) is the analytical standard of Opiranserin (hydrochloride) (HY-109067A). This product is intended for research and analytical applications. Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
|
-
- HY-155707
-
|
|
Dopamine Receptor
|
Inflammation/Immunology
|
|
MOR agonist-3 (Compound 84) is a D3R/MOR antagonist/partial agonist a(Ki 382 nM and 55.2 nM respectively). MOR agonist-3 has the potential to produce analgesic effects through MOR (μ-opioid receptor) (HY-149337) partial agonists. MOR agonist-3 can be used in the inflammation and neuropathic pain research .
|
-
- HY-17001
-
|
D 9998 Maleate
|
Potassium Channel
iGluR
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Flupirtine (D 9998) Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
|
-
- HY-W709349
-
|
D 9998 hydrochloride
|
Potassium Channel
iGluR
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Flupirtine (D 9998) hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
|
-
- HY-17001A
-
|
D 9998
|
Potassium Channel
iGluR
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Flupirtine (D 9998) is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
|
-
- HY-106605S
-
|
LY 120363-d8 hydrochloride
|
Isotope-Labeled Compounds
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Flumezapine-d8 (LY 120363-d8) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.
|
-
- HY-148502
-
|
|
mAChR
|
Neurological Disease
|
|
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) .
|
-
- HY-17001R
-
|
D 9998 Maleate (Standard)
|
Reference Standards
Potassium Channel
iGluR
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Flupirtine Maleate (Standard) is the analytical standard of Flupirtine Maleate (HY-17001). This product is intended for research and analytical applications. Flupirtine Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
|
-
- HY-W709349S
-
|
D 9998-d6 hydrochloride
|
Isotope-Labeled Compounds
Potassium Channel
iGluR
GABA Receptor
|
Neurological Disease
|
|
Flupirtine-d6 (D 9998-d6) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
|
-
- HY-110230
-
|
D 9998-d4 hydrochloride
|
Isotope-Labeled Compounds
Potassium Channel
iGluR
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Flupirtine-d4 (D 9998-d4) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
|
-
- HY-10233
-
|
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
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Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
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- HY-17001AR
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D 9998 (Standard)
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Reference Standards
Potassium Channel
iGluR
GABA Receptor
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Neurological Disease
Inflammation/Immunology
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Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
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- HY-159924
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Opioid Receptor
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Neurological Disease
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DBPR116 is a prodrug of BPRMU191 (HY-159923) with blood-brain barrier penetration capability. DBPR116 significantly improves the delivery of centrally targeted drugs. In combination with the antagonist Naltrexone (HY-76711), DBPR116 demonstrated superior safety and analgesic efficacy compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a prodrug strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing potential as a safer opioid analgesic .
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- HY-10233R
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Lu 02-030 hydrochloride (Standard); THIP hydrochloride (Standard)
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Reference Standards
GABA Receptor
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Neurological Disease
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Gaboxadol (hydrochloride) (Standard) is the analytical standard of Gaboxadol (hydrochloride). This product is intended for research and analytical applications. Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
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- HY-P1852
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Adenylate Cyclase
PTHR
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Neurological Disease
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TIP 39, Tuberoinfundibular Neuropeptide is an endogenous PTH2 receptor agonist and antihypertensive agent. TIP 39, Tuberoinfundibular Neuropeptide selectively activates the PTH2 receptor with no activity on the PTH1 receptor, stimulates cAMP production, activates adenylate cyclase, and elevates intracellular calcium levels via mobilization from intracellular stores. TIP 39, Tuberoinfundibular Neuropeptide is highly conserved in humans, mice, and rats. TIP 39, Tuberoinfundibular Neuropeptide is applicable to research related to nociception and inflammation-induced pain .
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- HY-101343
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5-HT Receptor
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Neurological Disease
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RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
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- HY-176710
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Protein Arginine Deiminase
Opioid Receptor
mAChR
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Neurological Disease
Inflammation/Immunology
Cancer
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PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca 2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .
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| Cat. No. |
Product Name |
Type |
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- HY-D1387
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Fluorescent Dyes
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Naloxone fluorescein acetate is the fluorescent-derivative of Naloxone. Naloxone is an opioid antagonist. Naloxone is the antidote for reversing the effects of an opioid overdose .
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| Cat. No. |
Product Name |
Type |
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- HY-W001874
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3-Hydrazinylpropanenitrile
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Biochemical Assay Reagents
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2-Cyanoethylhydrazine (3-Hydrazinylpropanenitrile) is a drug synthesis intermediate that can be used to synthesize an antagonist of opioid receptor-like 1 (ORL1) .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1852
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Adenylate Cyclase
PTHR
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Neurological Disease
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TIP 39, Tuberoinfundibular Neuropeptide is an endogenous PTH2 receptor agonist and antihypertensive agent. TIP 39, Tuberoinfundibular Neuropeptide selectively activates the PTH2 receptor with no activity on the PTH1 receptor, stimulates cAMP production, activates adenylate cyclase, and elevates intracellular calcium levels via mobilization from intracellular stores. TIP 39, Tuberoinfundibular Neuropeptide is highly conserved in humans, mice, and rats. TIP 39, Tuberoinfundibular Neuropeptide is applicable to research related to nociception and inflammation-induced pain .
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- HY-P1335
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CTAP
2 Publications Verification
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Opioid Receptor
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Neurological Disease
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CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-W013154
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Amino Acid Derivatives
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Others
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Fmoc-Tic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as the biotinylated derivative of the opioid receptor antagonist TIPP .
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- HY-P1335A
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Opioid Receptor
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Neurological Disease
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CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-P1329A
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Opioid Receptor
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Neurological Disease
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CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
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- HY-101230
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Opioid Receptor
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Neurological Disease
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ICI 174864 is a selective and brain-penetrant δ-opioid receptor antagonist with Ke values of 22.0 nM to 30.6 nM at δ-opioid receptor in mouse vas deferens. ICI 174864 selectively blocks biological effects mediated by the δ-opioid receptor agonist DPDPE (HY-P1334) after central administration. ICI 174864 reverses hypotension in rats with endotoxic shock and inhibits acetic acid-induced writhing in mice. ICI 174864 can be used for the research of opioid receptor subtypes, endotoxic hypotension and analgesic pathways .
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- HY-P1329
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Opioid Receptor
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Neurological Disease
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CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
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- HY-P1299A
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Opioid Receptor
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Neurological Disease
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UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
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- HY-P10395
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- HY-P10394
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- HY-P1299
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Opioid Receptor
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Neurological Disease
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UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
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- HY-P3839
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Opioid Receptor
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Neurological Disease
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Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
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- HY-P2669
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- HY-129422
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- HY-P10177
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Opioid Receptor
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Neurological Disease
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Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
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- HY-P10175
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Opioid Receptor
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Neurological Disease
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Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
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- HY-P2052
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Opioid Receptor
Neurokinin Receptor
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Others
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AWL 60 is a compound with SP antagonist and weak opioid agonist properties, which can antagonize SP-agonists in vitro and attenuate the decrease in blood pressure caused by SP-agonists in vivo.
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- HY-P5892
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Opioid Receptor
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Neurological Disease
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β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioid receptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .
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- HY-P2429
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Opioid Receptor
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Others
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N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a compound that can antagonize the δ-opioid receptor and the action of [D-Pen2,D-Pen ] enkephalin in vivo. Its antagonistic effect can be verified by specific behavioral experiments.
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-76711S
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Naltrexone-d4 is deuterium labeled Naltrexone (HY-76711). Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
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- HY-108229S
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6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
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- HY-B0188S
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Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
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- HY-123689S1
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Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
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- HY-17417AS
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Naloxone D5 is deuterium labeled Naloxone. Naloxone is a a potent opioid receptor antagonist.
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- HY-B0188AS
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Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
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- HY-W754114
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Nalmefene Sulfate-d3 is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders .
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- HY-123689S
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Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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- HY-A0118AS
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Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
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- HY-A0118S
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Naloxegol- 13C,d3 (NKTR-118- 13C,d3) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
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- HY-A0118S1
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Naloxegol- 13C,d2 (NKTR-118- 13C,d2) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
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- HY-W739948
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Naltrexone-d3 is a deuterated labeled Naltrexone (HY-76711) . Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system .
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- HY-106605S
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Flumezapine-d8 (LY 120363-d8) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.
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- HY-13243S1
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Alvimopan-d7 (ADL 8-2698-d7) is deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
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- HY-W709349S
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Flupirtine-d6 (D 9998-d6) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
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