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Opioid Receptor

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Opioid Receptor Signaling Pathway

Opioid Receptor Products

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  • Opioid Receptor Inhibitors (2)
  • Opioid Receptor Antagonists (5)
  • Opioid Receptor Agonists (5)
  • Opioid Receptor Modulator (1)
  • New Opioid Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2722 JTC-801 JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
Heliyon, 2024, 10(11):e32571
Sci Rep, 2023, 13(1):1483
Sci Rep, 2023, 13(1):1483
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
Front Neurosci, 2024, 18:1424936
Front Cell Infect Microbiol, 2023, 13:1139152
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
S2322 (+)-Matrine Matrine((+)-Matrine) is an alkaloid found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist.
J Vet Res, 2024, 68(1):35-44
Transl Oncol, 2023, 35:101712
Front Pharmacol, 2022, 13:1027441
S2503 Racecadotril Racecadotril (Acetorphan) is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM.
S0009 Asimadoline hydrochloride Asimadoline hydrochloride (EMD-61753 hydrochloride) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant).
E0472 BMS-986122 BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR), shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation, and potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes.
S5701 Alvimopan dihydrate (LY246736 dihydrate) Alvimopan (LY-246736) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.
E4647New Aticaprant Aticaprant (CERC-501, LY-2456302) is a potent, orally bioavailable, centrally-penetrant antagonist of the kappa opioid receptor with a Ki of 0.807 nM. It exhibits an antidepressant effect with the potential to treat major depressive disorder (MDD).
S5507 Trimebutine maleate Trimebutine maleate is the maleate salt form of trimebutine, which is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects.
E2868 Naloxegol Oxalate Naloxegol oxalate (NKTR-118 oxalate) is a μ-opioid-receptor antagonist with a Ki of 33.8 nM. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
S4588 Docusate Sodium Docusate Sodium (Aerosol OT, Bis(2-ethylhexyl) sulfosuccinate sodium salt, Constonate) is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally.
E2880 methylnaltrexone bromide Methylnaltrexone bromide is an antagonist of µ-opioid receptor that reduces the viability of lung cancer cells by inhibiting Src activation.
S2085 Trimebutine Trimebutine (Mebutin) is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain.
S5935 Alvimopan Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.
Curr Issues Mol Biol, 2024, 46(7):6472-6488
S2503 Racecadotril Racecadotril (Acetorphan) is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM.
S5701 Alvimopan dihydrate (LY246736 dihydrate) Alvimopan (LY-246736) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.
S2722 JTC-801 JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
Heliyon, 2024, 10(11):e32571
Sci Rep, 2023, 13(1):1483
Sci Rep, 2023, 13(1):1483
E4647New Aticaprant Aticaprant (CERC-501, LY-2456302) is a potent, orally bioavailable, centrally-penetrant antagonist of the kappa opioid receptor with a Ki of 0.807 nM. It exhibits an antidepressant effect with the potential to treat major depressive disorder (MDD).
E2868 Naloxegol Oxalate Naloxegol oxalate (NKTR-118 oxalate) is a μ-opioid-receptor antagonist with a Ki of 33.8 nM. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
E2880 methylnaltrexone bromide Methylnaltrexone bromide is an antagonist of µ-opioid receptor that reduces the viability of lung cancer cells by inhibiting Src activation.
S5935 Alvimopan Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.
Curr Issues Mol Biol, 2024, 46(7):6472-6488
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
Front Neurosci, 2024, 18:1424936
Front Cell Infect Microbiol, 2023, 13:1139152
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
S2322 (+)-Matrine Matrine((+)-Matrine) is an alkaloid found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist.
J Vet Res, 2024, 68(1):35-44
Transl Oncol, 2023, 35:101712
Front Pharmacol, 2022, 13:1027441
S0009 Asimadoline hydrochloride Asimadoline hydrochloride (EMD-61753 hydrochloride) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant).
S5507 Trimebutine maleate Trimebutine maleate is the maleate salt form of trimebutine, which is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects.
S2085 Trimebutine Trimebutine (Mebutin) is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain.
E0472 BMS-986122 BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR), shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation, and potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes.
E4647New Aticaprant Aticaprant (CERC-501, LY-2456302) is a potent, orally bioavailable, centrally-penetrant antagonist of the kappa opioid receptor with a Ki of 0.807 nM. It exhibits an antidepressant effect with the potential to treat major depressive disorder (MDD).

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