Opioid Receptor

Choose Selective Opioid Receptor Inhibitors

Opioid Receptor Signaling Pathway Map

Opioid Receptor Signaling Pathways

Opioid Receptor Products

  • All (17)
  • Opioid Receptor Inhibitors (2)
  • Opioid Receptor Antagonists (4)
  • Opioid Receptor Agonists (8)
  • Opioid Receptor Modulators (2)
  • New Opioid Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
S2103 Naltrexone HCl Naltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence.
Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
J Neurosci, 2021, 41(37):7727-7741
Sci Rep, 2021, 11(1):9300
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Biochem Biophys Res Commun, 2021, 562:55-61
Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91
S3066 Naloxone HCl Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
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.
E0013New DAMGO

DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.

S1139 ADL5859 HCl ADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.
Expert Opin Inv Drugs, 2012, 21(11):1607-18
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.
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.
Leuk Lymphoma, 2021, 1-10
J Med Virol, 2019, 91(8):1440-1447
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294) 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.
bioRxiv, 2020, 2020/9/20.4.7.30734
Exp Ther Med, 2019, 17(2):1312-1320
Nutrients, 2017, 9(12)
S3204 Meptazinol HCl Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM.
S5087 Tianeptine Tianeptine (S-1574, JNJ-39823277, TPI-1062) is an antidepressant agent that act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors.
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.
S2917New Cutamesine Dihydrochloride Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
S3972 Lobeline hydrochloride Lobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors.
J Cell Mol Med, 2020, 10.1111/jcmm.16029
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.
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.
S2103 Naltrexone HCl Naltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence.
Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
J Neurosci, 2021, 41(37):7727-7741
Sci Rep, 2021, 11(1):9300
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Biochem Biophys Res Commun, 2021, 562:55-61
Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91
S3066 Naloxone HCl Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
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.
E0013New DAMGO

DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.

S1139 ADL5859 HCl ADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.
Expert Opin Inv Drugs, 2012, 21(11):1607-18
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.
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.
Leuk Lymphoma, 2021, 1-10
J Med Virol, 2019, 91(8):1440-1447
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294) 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.
bioRxiv, 2020, 2020/9/20.4.7.30734
Exp Ther Med, 2019, 17(2):1312-1320
Nutrients, 2017, 9(12)
S3204 Meptazinol HCl Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM.
S5087 Tianeptine Tianeptine (S-1574, JNJ-39823277, TPI-1062) is an antidepressant agent that act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors.
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.
S2917New Cutamesine Dihydrochloride Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
S3972 Lobeline hydrochloride Lobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors.
J Cell Mol Med, 2020, 10.1111/jcmm.16029
E0013New DAMGO

DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.

S2917New Cutamesine Dihydrochloride Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.