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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.

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