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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 κ-selective agonist
Nalfurafine hydrochloride is a kappa-opioid receptor agonist- Lin Tian, .et al. , Research Square, 2023, May 30
- Alexander R French, .et al. , Pharmacol Biochem Behav, 2022, May;216:173377 PMID: 35364122
- Wen-Wen Zhang, .et al. , JCI Insight, 2022, Feb 8;7(3):e153191 PMID: 34914639
- A Dunn, .et al. , Psychopharmacology (Berl), 2020, May 20 PMID: 32435819
- Dunn AD, .et al. , ACS Chem Neurosci, 2019, Aug 21;10(8):3590-3600 PMID: 31313902
- Anika Mann, .et al. , Sci Signal, 2019, Mar 26;12(574). pii: eaau8072 PMID: 30914485
- Snyder LM, .et al. , Neuron, 2018, Sep 19;99(6):1274-1288.e6 PMID: 30236284
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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
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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 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. -
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.