Search Result
Results for "
kappa opioid receptors
" in MedChemExpress (MCE) Product Catalog:
10
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101718
-
-
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- HY-B0188A
-
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Org GB 94
|
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
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Neurological Disease
Metabolic Disease
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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 .
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-
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- HY-76711
-
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Opioid Receptor
|
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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-
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- HY-10487
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-
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- HY-P1333
-
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
|
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Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
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- HY-13243
-
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ADL 8-2698; LY 246736
|
Opioid Receptor
|
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-100903
-
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nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
|
Opioid Receptor
|
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
|
Opioid Receptor
|
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-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 .
|
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- HY-101302
-
|
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Opioid Receptor
TRP Channel
|
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-12363
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U-69593
1 Publications Verification
|
Opioid Receptor
|
Neurological Disease
|
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U-69593 is a potent and selective κ1-opioid receptor agonist . U-69593 attenuates addictive agent-induced behavioral sensitization in the rat . U-69593 reduces anxiety and enhances spontaneous alternation memory in mice . U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum .
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- HY-P3445A
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-
-
- HY-P2159
-
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Opioid Receptor
Endogenous Metabolite
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Neurological Disease
|
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Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .
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- HY-100845
-
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Divinorin A
|
Opioid Receptor
|
Cardiovascular Disease
|
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Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with Ki value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.
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- HY-P3445
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-
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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-P3609
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CR 665
2 Publications Verification
JNJ 38488502; FE 200665
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Opioid Receptor
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Neurological Disease
|
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CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
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- HY-P0088
-
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Dynorphin A Porcine Fragment 1-13
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Opioid Receptor
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Others
|
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Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
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- HY-107749
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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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- HY-P1337
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-
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- HY-107747
-
-
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- HY-76711S
-
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Isotope-Labeled Compounds
Opioid Receptor
|
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-15691
-
|
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Opioid Receptor
mTOR
|
Neurological Disease
Metabolic Disease
|
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PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
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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-P1594A
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Opioid Receptor
iGluR
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Neurological Disease
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Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-N0050
-
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(+)-Allomatrine
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Others
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Neurological Disease
|
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Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors .
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- HY-101205
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-
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- HY-15997B
-
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(±)-Trans-(1R,2R)-U-50488 hydrochloride
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Opioid Receptor
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Neurological Disease
|
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(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .
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- HY-101079
-
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Opioid Receptor
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Neurological Disease
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BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .
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- HY-121800
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-
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- HY-P1337A
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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-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-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-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-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-10486
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- HY-156614
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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-19231
-
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Org 41793
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Opioid Receptor
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Neurological Disease
|
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DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively. DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .
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- HY-15997C
-
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(±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride
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Opioid Receptor
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Neurological Disease
|
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(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .
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- HY-105235
-
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CI-977
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Opioid Receptor
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Neurological Disease
|
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Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
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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-151811
-
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Opioid Receptor
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Neurological Disease
|
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NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .
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-
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- HY-145128
-
-
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- HY-P1594
-
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Opioid Receptor
iGluR
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Neurological Disease
|
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Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-16765
-
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TD-1211
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Opioid Receptor
|
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-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-76657
-
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ADL 8-2698 monohydrate; LY 246736 monohydrate
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Opioid Receptor
|
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-135698
-
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M-CAM
|
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-122189
-
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(-)-Akuammine; Vincamajoridine
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Others
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Neurological Disease
|
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Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC50s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.
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- HY-171758
-
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Opioid Receptor
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Neurological Disease
|
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BU72 is a highly potent and long-acting agonist of μ and κ opioid receptors, and also has a partial agonist effect on δ opioid receptors (EC50 values are 0.054, 0.033, and 0.58 nM, respectively). BU72 has a strong and long-lasting analgesic effect, which is mainly mediated by μ opioid receptors. BU72 has a long-lasting activity and can partially reverse the analgesic effect of morphine. BU72 can be used in the study of opioid dependence .
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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-136786
-
-
- HY-P0186
-
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Opioid Receptor
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Neurological Disease
|
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Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
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- HY-108043
-
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Opioid Receptor
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Neurological Disease
|
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AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (Ki of 0.49 and 0.75 nM and EC50 of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .
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- HY-B0188AS
-
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Org GB 94-d3
|
Isotope-Labeled Compounds
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
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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 .
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- HY-P10203
-
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Opioid Receptor
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Inflammation/Immunology
|
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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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-P10006
-
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Opioid Receptor
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Neurological Disease
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Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
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- HY-15691A
-
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Opioid Receptor
mTOR
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Neurological Disease
Metabolic Disease
|
|
PF-4455242 hydrochloride is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-4455242 hydrochloride blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-4455242 hydrochloride promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-4455242 hydrochloride attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-4455242 hydrochloride can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
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- HY-P3376
-
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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 .
|
-
- HY-169822
-
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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
|
Neurological Disease
|
|
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-117881
-
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Opioid Receptor
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Neurological Disease
|
|
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 .
|
-
- HY-130482
-
-
- HY-122169
-
|
Ketocyclazocine
|
Opioid Receptor
|
Neurological Disease
|
|
Ketazocine (Ketocyclazocine) is a selective κ-opioid receptor (KOR) agonist. Ketazocine is promising for research of analgesics and sedatives .
|
-
- HY-160761
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
|
-
- HY-16765A
-
|
TD-1211 sulfate
|
Opioid Receptor
|
Neurological Disease
|
|
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.
|
-
- HY-107747A
-
-
- HY-118615
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-107748A
-
|
5'-GNTI TFA
|
Endogenous Metabolite
|
Neurological Disease
|
|
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 .
|
-
- HY-P1333A
-
|
|
Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
|
Neurological Disease
|
|
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
|
-
- HY-19206
-
-
- HY-167842
-
-
- HY-107750
-
-
- HY-141468
-
|
β-CNA dihydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term opioid receptor blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception .
|
-
- HY-163017
-
-
- HY-123389
-
|
(R)-UM-1071
|
Opioid Receptor
|
Endocrinology
|
|
MR2034 ((R)-UM-1071) is a κ-opioid receptor agonist with activity that stimulates the hypothalamic-pituitary-adrenal axis. MR2034 has shown the potential to promote mood and inhibit addictive behaviors in animal models and can be used to study inhibitory approaches related to mood and addictive disorders. MR2034 is selective for κ-opioid receptors and can effectively modulate biological processes related to stress and mood .
|
-
- HY-100963
-
-
- HY-177790
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
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 .
|
-
- HY-13243R
-
|
ADL 8-2698 (Standard); LY 246736 (Standard)
|
Opioid Receptor
Reference Standards
|
Neurological Disease
Cancer
|
|
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 .
|
-
- HY-101205A
-
-
- HY-105235A
-
|
CI-977 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
|
-
- HY-P1625
-
|
Dynorphin A ethylamide (1-9)
|
Opioid Receptor
|
Neurological Disease
|
|
Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
|
-
- HY-163917
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .
|
-
- 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-182453
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
RM1490 (Compound 251) acts as an inhibitor of μ-opioid receptor (MOR) (IC50 ≤ 300 nM), an activator of δ-opioid receptor (DOR) (EC50 > 3000 nM), and an inhibitor of κ-opioid receptor (KOR) (IC50 ≤ 300 nM). RM1490 is applicable to the research of neuropsychiatric disorders .
|
-
- HY-180212
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SYK-1106 is a potent delta-opioid receptor (DOR) agonist with an EC50 of 89 pM and a Ki of 848 pM. SYK-1106 is selective for μ and κ opioid receptors, with Ki values of 9.54 nM and 2.45 nM, respectively. SYK-1106 induces dose-dependent antidepressant-like effects. SYK-1106 can be used for the research of depression .
|
-
- HY-183773
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus .
|
-
- HY-100903R
-
|
nor-Binaltorphimine dihydrochloride (Standard); nor-BNI dihydrochloride (Standard)
|
Opioid Receptor
Reference Standards
|
Neurological Disease
|
|
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 .
|
-
- HY-179282
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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) .
|
-
- HY-13597
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CJ-15161 is a κ-opioid receptor agonist. CJ-15161 can be used to study physiological functions such as pain relief and emotional regulation .
|
-
- 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.
|
-
- HY-N12302A
-
|
(E/Z)-N1-Dihydrocaffeoyl, N10-caffeoyl spermidine
|
Drug Derivative
|
Others
|
|
(E/Z)-Scotanamine D is a hydroxycinnamic acid amide found in the roots of Scopolia tangutica. (E/Z)-Scotanamine D is inactive against μ-, δ-, and κ-opioid receptors .
|
-
- HY-13243S1
-
|
ADL 8-2698-d7; LY 246736-d7
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
Cancer
|
|
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 .
|
-
- HY-163916
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SalA-VS-07 is a G protein-biased partial agonist for the Kappa-opioid receptor (KOR). SalA-VS-07 can be used for research of pain and other disorders .
|
-
- HY-120949
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
(1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .
|
-
- HY-135230
-
|
FP3FBZ
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-P0186A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
|
-
- HY-A0115R
-
|
HOE 498 diacid (Standard); Ramipril diacid (Standard)
|
Drug Metabolite
Reference Standards
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-76657AR
-
|
ADL 8-2698 dihydrate (Standard); LY 246736 dihydrate (Standard)
|
Reference Standards
Opioid Receptor
|
Neurological Disease
Cancer
|
|
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 .
|
-
- 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-107749R
-
|
|
Reference Standards
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-P992012
-
|
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
CA1001 is a small-molecule ZNF74 inhibitor and a peripherally restricted κ/δ dual opioid receptor agonist. CA1001 exhibits potent antitumor activity both in vitro and in vivo. CA1001, in combination with immune checkpoint inhibitors, significantly enhances tumor regression. CA1001 activates peripherally restricted κ/δ dual opioid receptors and exerts analgesic effects under conditions of inflammatory pain, neuropathic pain, and mechanical hyperalgesia. CA1001 can be used in research related to melanoma, mechanical hyperalgesia, neuropathic pain, and inflammatory arthritis pain.
|
-
- HY-136654
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
LPK-26 hydrochloride is a selective kappa-opioid receptor agonist with a Ki of 0.68 nM. LPK-26 exhibits potent antinociceptive effects with low physical dependence potential and can be utilized in relevant research .
|
-
- HY-17609
-
|
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-11052A
-
|
|
Opioid Receptor
|
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 .
|
-
- HY-137920
-
|
|
Opioid Receptor
|
Cardiovascular Disease
|
|
Salvinorin A (Divinorin A) propionate is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with Ki value of 4.3 nm. Salvinorin A propionate is a non-nitrogenous neoclerodane isolated from Salvia divinorum .
|
-
- 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-136208
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-171236
-
|
|
Opioid Receptor
|
|
|
FEKAP is a brain-penetrant and selective kappa opioid receptor (KOR) agonist (Ki = 0.43 nM) which isotope labeled form exhibits excellent imaging properties. 11C-FEKAP can be utilized as a radiotracer for imaging KOR .
|
-
- HY-P3647
-
-
- HY-P3647A
-
|
|
Opioid Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .
|
-
- HY-W019787
-
|
|
Opioid Receptor
CXCR
|
Neurological Disease
|
|
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
|
-
- HY-P5892
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-101718R
-
|
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.
|
-
- HY-P5907
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
- HY-17609C
-
|
CR-845 acetate; FE-202845 acetate
|
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin (CR-845; FE-202845) acetate is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin acetate produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-19627A
-
|
S-297995 tosylate
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
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 .
|
-
- HY-19627
-
|
S-297995
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
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 .
|
-
- HY-P1316A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
|
-
- HY-P1316
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
|
-
- 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-124959
-
|
U-62066 mesylate
|
Opioid Receptor
|
Neurological Disease
|
|
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-106756
-
|
U-62066
|
Opioid Receptor
|
Neurological Disease
|
|
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-P0185
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
|
-
- HY-P0185A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
|
-
- HY-105389
-
|
RWJ-38705
|
Opioid Receptor
|
Neurological Disease
|
|
Tramadol N-oxide (RWJ 38705) is an analgesic. Tramadol N-oxide sproduces dose-related, long-lasting antinociception. Tramadol N-oxide has affinity for μ opioid receptor (Ki = 38.5 μM) and δ, κ receptors (Ki > 100 μM). Tramadol N-oxide can be used for the study of analgesic effect .
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- HY-P1299A
-
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Opioid Receptor
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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 .
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-
- HY-176710A
-
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Drug Isomer
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Others
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(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).
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-
- HY-133173
-
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RU51599
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Vasopressin Receptor
Opioid Receptor
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Neurological Disease
|
|
Niravoline (RU51599) is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. Niravoline has a pure water diuresis effect without associated electrolyte excretion. Niravoline can reduce brain oedema following transient forebrain ischaemia in rats .
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-
- HY-106605
-
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LY 120363
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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 .
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- HY-111011
-
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JNJ 38488502 acetate; FE 200665 acetate
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Opioid Receptor
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Neurological Disease
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|
CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.
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- HY-P3634
-
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Opioid Receptor
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Neurological Disease
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|
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .
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- HY-126910
-
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Opioid Receptor
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Metabolic Disease
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|
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .
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- HY-170973
-
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Opioid Receptor
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KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
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- HY-156131
-
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ADL 2-1294
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Opioid Receptor
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Neurological Disease
Inflammation/Immunology
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|
Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with Ki valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE2 (HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea .
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- HY-129668
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Adrenergic Receptor
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Neurological Disease
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|
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 .
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- HY-136832
-
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|
Serotonin Transporter
Potassium Channel
Arrestin
Opioid Receptor
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Cardiovascular Disease
Neurological Disease
|
|
Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .
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-
- HY-110302
-
|
|
Opioid Receptor
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Neurological Disease
|
|
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
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-
- HY-118949
-
|
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Opioid Receptor
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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 .
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-
- HY-P1301
-
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Opioid Receptor
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Neurological Disease
|
|
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
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-
- HY-P4679
-
|
E2078
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Opioid Receptor
|
Neurological Disease
|
|
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .
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-
- HY-163277
-
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Opioid Receptor
|
Inflammation/Immunology
|
|
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
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-
- HY-130696
-
|
(+)-Trans-(1R,2R)-U-50488
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Opioid Receptor
|
Neurological Disease
|
|
(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
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-
- HY-15997A
-
|
(+)-Trans-(1R,2R)-U-50488 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
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-
- HY-P1301A
-
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Opioid Receptor
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Neurological Disease
|
|
[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
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-
- 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.
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-
- HY-181515
-
|
|
Opioid Receptor
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Neurological Disease
|
|
KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research .
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-
- HY-106131
-
|
PD-123497
|
Sodium Channel
Opioid Receptor
|
Cardiovascular Disease
|
|
RSD-921 (PD-123497) is a potent Na + channel blocker with anti-arrhythmic activity. RSD-921 displays a low affinity for κ-opioid receptors and behaves as a weak κ-agonist in vitro. RSD 921 displays state-, time- and voltage-dependent block of the open state of cardiac, skeletal muscle and neuronal Na + channels expressed in Xenopus oocytes. RSD-921 can be used for cardiac arrhythmias research .
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-
- HY-159088
-
|
|
Opioid Receptor
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Neurological Disease
|
|
KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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-
- HY-161812
-
|
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Opioid Receptor
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Others
|
|
MOR agonist-4 (2d) is a G protein signaling-biased Kappa opioid receptor (KOR) agonist with an EC50 value of 11 nM. MOR agonist-4 contains an electron withdrawing CF3 group and a bias factor of 38 based on triazole. MOR agonist-4 is used in the research of pruritis and analgesia .
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-
- HY-130696A
-
|
(±)-trans-(1R,2R)-U-50488
|
Opioid Receptor
|
Neurological Disease
|
|
(±)-U-50488 ((±)-trans-(1R,2R)-U-50488) is a selective kappa opioid receptor agonist. (±)-U-50488 can improve symptoms related to status epilepticus, but has no significant effect on spontaneous seizure episodes. (±)-U-50488 can be used for research of epilepsy .
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-
- HY-135238
-
|
PD-117302
|
Opioid Receptor
|
Others
|
|
(rel)-RSD 921 (PD-117302) is a κ-opioid receptor agonist. (rel)-RSD 921 did not have a greater food-inducing effect in obese than in lean Zucker rats; in both obese and lean Zucker rats, lean rats were more sensitive to its initial food-inducing effect but ultimately ate less.
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-
- HY-16979
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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-P1300
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
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-
- HY-145404
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-17609S
-
|
CR-845-d5; FE-202845-d5
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-17609S1
-
|
CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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-
- HY-P1300A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
-
- 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-178945
-
|
|
Opioid Receptor
Interleukin Related
TNF Receptor
Sigma Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation .
|
-
- HY-110252
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC50 of 248 nM and Ki of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety .
|
-
- HY-15997
-
|
(-)-Trans-(1S,2S)-U-50488 hydrochloride
|
Opioid Receptor
|
Infection
Cancer
|
|
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM) .
|
-
- HY-178720
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SHR0687 is a selective tetrapeptide kappa opioid receptor (KOR) agonist with an EC50 of 0.53 pM. SHR0687 displays high potency and selectivity over MOR and DOR, with negligible blood-brain barrier penetration. SHR0687 activates KOR specifically, leading to potential modulation of neurological pathways without significant central nervous system effects. SHR0687 can be used for the research of pain .
|
-
- HY-N0164
-
Matrine
Maximum Cited Publications
18 Publications Verification
Matridin-15-one; Vegard; α-Matrine
|
PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- 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-N0164R
-
|
Matridin-15-one (Standard); Vegard (Standard); α-Matrine (Standard)
|
PINK1/Parkin
Reference Standards
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- HY-130118
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
|
MRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC50=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. MRGPRX1 agonist 1 is inactive against MRGPRC11. MRGPRC11 inhibits high voltage-activated (HVA) Ca 2+ currents, reduces neurotransmitter release, and mitigates nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is useful for the study of chronic pain, especially neuropathic pain .
|
-
- HY-120045A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DuP 747 hydrochloride is an analgesic with selective kappa-opioid receptor agonist activity. DuP 747 showed less spiradoline-appropriate selection when administered SC, but showed a partial generalized response to spiradoline when administered IP or PO. The 5-hydroxy-desmethoxy metabolite of DuP 747 induced selection of the saline-appropriate lever only. The effects of DuP 747 suggest that its metabolites may play a major role in the similar responses to spiradoline after IP and PO administration .
|
-
- HY-W654256
-
|
Matridin-15-one-d3; Vegard-d3; α-Matrine-d3
|
Isotope-Labeled Compounds
PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Matrine-d3 (Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- HY-120511
-
KNT-127
1 Publications Verification
|
Opioid Receptor
|
Neurological Disease
|
|
KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (Ki = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases .
|
-
- HY-P11642
-
|
|
ERK
Androgen Receptor
Opioid Receptor
Enteropeptidase
mTOR
Aminopeptidase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
|
-
- HY-176710
-
|
|
Protein Arginine Deiminase
Opioid Receptor
mAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-P11642A
-
|
|
Enteropeptidase
Aminopeptidase
Opioid Receptor
ERK
mTOR
Androgen Receptor
|
Inflammation/Immunology
|
|
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
|
-
- HY-175532
-
|
|
mAChR
|
Neurological Disease
|
|
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
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-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-17609
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CR-845; FE-202845
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Opioid Receptor
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Neurological Disease
Inflammation/Immunology
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Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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- HY-P1333
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
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- HY-P0185
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Opioid Receptor
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Neurological Disease
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Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
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- HY-P3445A
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- HY-P2159
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Opioid Receptor
Endogenous Metabolite
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Neurological Disease
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Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .
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- HY-P3445
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- HY-P3609
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CR 665
2 Publications Verification
JNJ 38488502; FE 200665
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Opioid Receptor
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Neurological Disease
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CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
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- HY-P0088
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Dynorphin A Porcine Fragment 1-13
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Opioid Receptor
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Others
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Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
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- HY-P1337
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- HY-P0186A
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Opioid Receptor
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Neurological Disease
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Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
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- HY-P1594A
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Opioid Receptor
iGluR
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Neurological Disease
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Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-P1337A
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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-P1594
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Opioid Receptor
iGluR
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Neurological Disease
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Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-P0186
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Opioid Receptor
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Neurological Disease
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Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
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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-W019787
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Opioid Receptor
CXCR
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Neurological Disease
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BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
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- HY-P5907
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Opioid Receptor
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Neurological Disease
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Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
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- HY-P1316A
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Opioid Receptor
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Neurological Disease
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Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
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- HY-P0185A
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Opioid Receptor
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Neurological Disease
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Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
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- HY-P11642A
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Enteropeptidase
Aminopeptidase
Opioid Receptor
ERK
mTOR
Androgen Receptor
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Inflammation/Immunology
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Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
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- HY-P10203
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Opioid Receptor
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Inflammation/Immunology
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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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-P10006
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Opioid Receptor
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Neurological Disease
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Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
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- HY-P3376
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- HY-P1333A
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
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- HY-P1625
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Dynorphin A ethylamide (1-9)
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Opioid Receptor
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Neurological Disease
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Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
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- HY-P3647
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- HY-P3647A
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Opioid Receptor
Adenylate Cyclase
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Neurological Disease
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[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .
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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-P1316
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Opioid Receptor
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Neurological Disease
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Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
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- HY-P3634
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Opioid Receptor
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Neurological Disease
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[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .
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- HY-P1301
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Opioid Receptor
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Neurological Disease
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[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
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- HY-P4679
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E2078
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Opioid Receptor
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Neurological Disease
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(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .
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- HY-P1301A
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Opioid Receptor
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Neurological Disease
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[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
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- HY-P1300
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Opioid Receptor
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Neurological Disease
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[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
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- HY-P1300A
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Opioid Receptor
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Neurological Disease
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[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
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- HY-P11642
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ERK
Androgen Receptor
Opioid Receptor
Enteropeptidase
mTOR
Aminopeptidase
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Neurological Disease
Inflammation/Immunology
Cancer
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Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P992012
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Opioid Receptor
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Neurological Disease
Cancer
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CA1001 is a small-molecule ZNF74 inhibitor and a peripherally restricted κ/δ dual opioid receptor agonist. CA1001 exhibits potent antitumor activity both in vitro and in vivo. CA1001, in combination with immune checkpoint inhibitors, significantly enhances tumor regression. CA1001 activates peripherally restricted κ/δ dual opioid receptors and exerts analgesic effects under conditions of inflammatory pain, neuropathic pain, and mechanical hyperalgesia. CA1001 can be used in research related to melanoma, mechanical hyperalgesia, neuropathic pain, and inflammatory arthritis pain.
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(5)
| 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-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-17609S1
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Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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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-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-17609S
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Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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- HY-W654256
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Matrine-d3 (Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
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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-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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