BMS 986122 CAS NO.313669-88-4

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BMS 986122 is a positive allosteric modulator of the μ-Opioid receptor. It significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by an EC10 (30 pM) concentration of endomorphin-I in CHO-μ cells. BMS 986122 potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human recombinant μ-opioid receptors with EC50 of 8.9 μM. It also enhances [35S]GTPγ binding stimulated by the μ-opioid agonist DAMGO by 7- and 4.5-fold in C6μ glioma cell membranes.