mumumu-opioid-receptor Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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.

Selective μ-opioid receptor, Ki: 3.3 nM
S2103 Naltrexone HCl

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

Selective opioid receptor, IC50: 8 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.

Selective μ-opioid receptor, Ki: 383 nM
S2503 Racecadotril

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

Selective
S3066 Naloxone HCl

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

Selective
S3204 Meptazinol HCl

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

Selective
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.

Pan μ-opioid receptor, Ki: 0.77 nM
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.

Pan μ-opioid receptor, Ki: 0.77 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.

Pan μ-opioid receptor, Ki: 32 nM