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NOP receptor agonist
MCOPPB is a compound which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07. -
Opioid Receptor agonist
ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM. -
Opioid Receptor antagonist
JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.- Lihao Gu, .et al. , Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. , Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
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Opioid Receptors agonist
BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM). -
Opioid antagonist
Alvimopan behaves as a peripherally acting μ-opioid antagonist. Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract. -
KOR antagonist
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception. -
Opioid Receptor Agonist
Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist -
dopamine receptor agonist
Nalmefene hydrochloride is an opioid receptor antagonist.- Mark G Papich, .et al. , Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
- Dynorphin A (1-13) Acetate is a potent, endogenous ??-agonist.
- E J Kuijer, .et al. , Neuropharmacology, 2025, Jul 1:272:110407 PMID: 40074169
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μ-opioid receptor agonist
Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. -
μ-opioid receptor agonist
Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. -
μ-opioid antagonist
Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation. -
Opioid antagonist
Naloxegol is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. - Docusate Sodium 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.
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MOR agonist
SR17018 is an mu-opioid-receptor (MOR) agonist with an EC50 of 97 nM.- Rob Hill, .et al. , Br J Pharmacol, 2023, Jul 24 PMID: 37489013
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KOR agonist
Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively). -
opioid receptor antagonis
Bevenopran, also known as CB-5945, ADL-5945, MK-2402, OpRA III, is a peripherally selective μ- and δ-opioid receptor antagonist. -
μ- opioid receptor agonist
Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome. -
κ opioid receptor antagonist
BTRX-335140 (CYM-53093) is a potent and selective, 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. -
μ-opioid receptor antagonist
GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. -
NOP receptor antagonist
LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models. -
kappa opioid agonist
ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye. -
kappa opioid receptor antagonist
Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM. -
NOP agonist
MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention. -
δ opioid receptor antagonist
Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM. -
μ-opioid receptor (MOR) antagonist
GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. -
mu-opioid receptor agonist
CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively. -
μ-opioid receptor (MOR) antagonist
GSK1521498 hydrochloride is a potent and selective μ-opioid receptor (MOR) antagonist.
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δ opioid receptor agonist
AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2??0.9 nM for δ agonist potency. -
non-peptide nociceptin receptor (NOP) agonist
MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention. -
δ-opioid receptor modulator
BMS-986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor. -
δ-opioid receptor modulator
BMS-986187 is a potent and selective positive allosteric modulator (PAM) of the δ-opioid receptor and a G-protein-biased allosteric agonist. - Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
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μ-opioid receptor agonist
Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain. -
opioid κ-receptor agonist
Dynorphin B (1-13) acts as an agonist on opioid κ-receptor. - Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
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Opioid Receptor Agonist
BPR1M97 is a dual-acting agonist for the mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor, exhibiting Ki values of 1.8 nM and 4.2 nM, respectively. This compound demonstrates significant potency and effective penetration of the blood-brain barrier, resulting in pronounced antinociceptive effects. BPR1M97 serves as a useful tool for research in pain management and opioid receptor biology. -
κ-opioid agonists
ICI-204448 is a κ-opioid receptor agonist that demonstrates limited central nervous system penetration. This compound effectively displaces the binding of the κ-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes. It is valuable for research applications focused on the role of κ-opioid receptors in pain modulation and neuropharmacology studies. -
μ Opioid Receptor Agonist
Loperamide is a selective μ opioid receptor agonist with Ki values of 3, 48, and 1156 nM for μ, δ, and κ opioid receptors, respectively. It demonstrates significant antinociceptive and antihyperalgesic properties, along with peripheral selectivity that enhances fluid, electrolyte, and glucose absorption. Loperamide effectively mitigates intestinal secretion induced by PGE2 and cholera toxin while reducing intestinal motility. This compound is applicable in research focused on inflammatory pain and chronic diarrhea.

