Opioid Receptor

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S4501

Naloxone HCl Dihydrate

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

S4588New

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.

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.

S2503

Racecadotril

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

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.

S3204

Meptazinol HCl

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

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.

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.

2016, 80:16-22

2016, 92(5):728-34

S2103

Naltrexone HCl

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

2014, 4:7270

2015, 10.1111/phpp.12231

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.

2014, 58(8):4875-84

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.

2012, 21(11):1607-18

S2503

Racecadotril

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

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.

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
S4501

Naloxone HCl Dihydrate

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

Catalog No. Information Product Use Citations Product Validations
S4588New

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.