Home GPCR & G Protein Opioid Receptor

Opioid Receptor

Opioid receptors, which belong to G-protein-coupled super family, include mu-opioid receptor, delta-opioid receptor, and kappa-opioid receptor. Opioid receptors are receptor for opiate drugs. Opioid receptors can be found in the mammalian central nervous system and some other tissues, including the immune system. After opiate drugs binding to the specific receptor sites of opioid receptors, opioid receptors can executive function such as analgesia, sedation and so on.

Other GPCR & G Protein Related Inhibitors

Hedgehog/Smoothened PKA CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor SGLT GPR CCR MT Receptor

Isoform-selective Products

Cat.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.
Clin Exp Med, 2025, 26(1):11
Cancer Drug Resist, 2025, 8:45
Heliyon, 2024, 10(11):e32571
Verified customer review of JTC-801
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.
Cancer Cell, 2025, 43(4):776-796.e14
Front Neurosci, 2024, 18:1424936
Front Cell Infect Microbiol, 2023, 13:1139152
Verified customer review of Loperamide HCl
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 Immunother Cancer, 2025, 13(6)e011716
J Vet Res, 2024, 68(1):35-44
Transl Oncol, 2023, 35:101712
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.
E4647 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.

Signaling Pathway Map