Search Result
Results for "
opioid antagonist
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-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-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-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-107744
-
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Opioid Receptor
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Neurological Disease
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Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence .
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-
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- HY-120277
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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-17417A
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Opioid Receptor
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Neurological Disease
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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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-
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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-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 .
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- HY-10486
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-
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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
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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-A0118A
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NKTR-118 oxalate; AZ-13337019 oxalate
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Opioid Receptor
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Neurological Disease
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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-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 is a potent and selective κ opioid receptor antagonist.
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- HY-156614
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-
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- HY-17417
-
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Opioid Receptor
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Neurological Disease
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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-112263
-
-
-
- HY-100122
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-
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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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-
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- HY-A0118AS
-
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Isotope-Labeled Compounds
Opioid Receptor
|
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[1][2].
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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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-
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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-101233
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M 154129
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ICI 154 129 is a delta-opioid receptor antagonist and can be used for seizure research.
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- HY-101718
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-
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- HY-107749
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-
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- HY-101306
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Clocinnamox (mesylate) is a potent opioid antagonist acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors .
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- HY-117040
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Norbinaltorphimine; NorBNI
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Opioid Receptor
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Others
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nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo .
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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-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-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-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-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-10487
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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-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-101011
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-
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- HY-114072A
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-
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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-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-13274
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- HY-19902
-
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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-155707
-
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Others
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Inflammation/Immunology
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MOR agonist-3 (Compound 84) is a D3R/MOR antagonist (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 and to reduce opioid abuse through D3R antagonists. MOR agonist-3 can be used in the treatment of inflammation and neuropathic pain research .
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- HY-101223
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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-P1335
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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-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-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-17001
-
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Potassium Channel
iGluR
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Neurological Disease
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Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties .
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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-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-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
|
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-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-A0142
-
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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-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-15708
-
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Opioid Receptor
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Neurological Disease
|
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-11052A
-
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Opioid Receptor
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Neurological Disease
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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-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-124754
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BTRX-335140; CYM-53093
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Opioid Receptor
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Neurological Disease
Metabolic Disease
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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 .
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- HY-163065
-
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Opioid Receptor
Sigma Receptor
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Neurological Disease
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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 .
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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-P1299
-
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Opioid Receptor
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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 .
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- HY-118949
-
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Opioid Receptor
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Metabolic Disease
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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 .
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- HY-P3839
-
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Opioid Receptor
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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 .
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- HY-134189
-
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Opioid Receptor
Sigma Receptor
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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 .
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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-109067
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VVZ-149
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GlyT
5-HT Receptor
P2X Receptor
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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 .
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- HY-109067A
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VVZ-149 hydrochloride
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GlyT
5-HT Receptor
P2X Receptor
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Neurological Disease
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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 .
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- HY-134189A
-
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Sigma Receptor
Opioid Receptor
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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 .
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- HY-155706
-
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Opioid Receptor
Dopamine Receptor
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Inflammation/Immunology
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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 .
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- HY-119733
-
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-148502
-
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mAChR
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Neurological Disease
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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) .
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- HY-10233
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Lu 02-030 hydrochloride; THIP hydrochloride
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GABA Receptor
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Neurological Disease
|
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-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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Cat. No. |
Product Name |
Type |
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- HY-D1387
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Fluorescent Dyes/Probes
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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 |
Target |
Research Area |
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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-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-P1335
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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-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-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-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-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-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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Cat. No. |
Product Name |
Chemical Structure |
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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[1][2].
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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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