BMS 986122 is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).
CAS：313669-88-4
分子式：C16H15BrClNO3S2
分子量：448.8
纯度：98%
存储：Store at -20°C

Background:

BMS 986122 is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM). It potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human recombinant μ-opioid receptors (EC50 = 8.9 μM). BMS 986122 also enhances [35S]GTPγ binding stimulated by the μ-opioid agonist DAMGO by 7- and 4.5-fold in C6μ glioma cell membranes that express μ-opioid receptors and mouse brain membranes, respectively.