Opioid Receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S2480 Loperamide HCl <1 mg/mL 22 mg/mL 4 mg/mL
S3066 Naloxone HCl 72 mg/mL 72 mg/mL <1 mg/mL
S2722 JTC-801 <1 mg/mL 90 mg/mL 31 mg/mL
S1139 ADL5859 HCl 5 mg/mL 86 mg/mL 1 mg/mL
S2103 Naltrexone HCl 14 mg/mL 14 mg/mL <1 mg/mL
S5087 Tianeptine -1 mg/mL 87 mg/mL -1 mg/mL
S3972 Lobeline hydrochloride -1 mg/mL 74 mg/mL -1 mg/mL
S2503 Racecadotril <1 mg/mL 22 mg/mL 77 mg/mL
S4588 Docusate Sodium 18 mg/mL 88 mg/mL 88 mg/mL
S2322 (+)-Matrine 11 mg/mL 49 mg/mL 49 mg/mL
S2085 Trimebutine <1 mg/mL 50 mg/mL <1 mg/mL
S4714 (-)-Menthol 16 mg/mL 31 mg/mL 31 mg/mL
S3204 Meptazinol HCl 53 mg/mL 53 mg/mL 53 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

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.


Naloxone HCl

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



JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.


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.


Naltrexone HCl

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



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.


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.



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


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.



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.



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.



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


Meptazinol HCl

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