Opioid Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Opioid Receptor Products

New Opioid Receptor Products
Catalog No. Information Product Use Citations Product Validations
S5701New

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.

S2503

Racecadotril

Racecadotril is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM.

S3066

Naloxone HCl

Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose.

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.

S2103

Naltrexone HCl

Naltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence.

S5935New

Alvimopan

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.

S2480

Loperamide HCl

Loperamide HCl 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.

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.

S5507New

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.

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.

S2085

Trimebutine

Trimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain.

S5087

Tianeptine

Tianeptine 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.

S4714

(-)-Menthol

(-)-Menthol is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8.

S3204

Meptazinol HCl

Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM.

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.

S4588

Docusate Sodium

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.

Catalog No. Information Product Use Citations Product Validations
S5701New

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.

S2503

Racecadotril

Racecadotril is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM.

Catalog No. Information Product Use Citations Product Validations
S3066

Naloxone HCl

Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose.

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.

S2103

Naltrexone HCl

Naltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence.

S5935New

Alvimopan

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.

Catalog No. Information Product Use Citations Product Validations
S2480

Loperamide HCl

Loperamide HCl 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.

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.

S5507New

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.

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.

S2085

Trimebutine

Trimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain.

S5087

Tianeptine

Tianeptine 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.

S4714

(-)-Menthol

(-)-Menthol is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8.

S3204

Meptazinol HCl

Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM.

Catalog No. Information Product Use Citations Product Validations
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.

Catalog No. Information Product Use Citations Product Validations
S4588

Docusate Sodium

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.