Opioid Receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S5701 Alvimopan dihydrate (LY246736 dihydrate) -1 mg/mL 92 mg/mL -1 mg/mL
S2503 Racecadotril <1 mg/mL 22 mg/mL 77 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
S2103 Naltrexone HCl 14 mg/mL 14 mg/mL <1 mg/mL
S2480 Loperamide HCl <1 mg/mL 22 mg/mL 4 mg/mL
S1139 ADL5859 HCl 5 mg/mL 86 mg/mL 1 mg/mL
S5507 Trimebutine maleate -1 mg/mL 100 mg/mL -1 mg/mL
S5087 Tianeptine -1 mg/mL 87 mg/mL -1 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
S3972 Lobeline hydrochloride -1 mg/mL 74 mg/mL -1 mg/mL
S4588 Docusate Sodium 18 mg/mL 88 mg/mL 88 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

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.



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


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.


Naltrexone HCl

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


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.


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.


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.



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.



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.


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.


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.