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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
CCI-1008 is an opioid receptor agonist that exhibits significant activity in targeting the µ-opioid receptor. It is primarily utilized in research related to nervous system diseases, exploring mechanisms of pain modulation and addiction. This compound serves as a valuable tool for investigating therapeutic strategies aimed at managing pain and opioid-related disorders. -
κ Opioid Receptor Antagonist
Norbinaltorphimine dihydrochloride selectively antagonizes the κ-opioid receptor, making it an important tool for research on opioid signaling pathways. Its potent inhibitory action allows for the investigation of κ-opioid receptor-related biological processes and potential therapeutic applications in pain management and addiction studies. Researchers can utilize this compound to explore the effects of opioid receptor modulation in various experimental settings. -
Opioid receptor Antagonist
Naloxone is an antagonist of opioid receptors, primarily acting to reverse the effects of opioid overdose. It effectively alleviates respiratory depression caused by opioid toxicity, restoring normal breathing. Research applications include studies on opioid overdose treatment, respiratory pharmacodynamics, and the examination of opioid receptor interactions. Naloxone may also induce pulmonary edema and cardiac arrhythmias as potential side effects.

