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BMS-986122

CAS No. : 313669-88-4

MCE 站：BMS-986122

产品活性：BMS-986122 是一种选择性的、有效的μ-阿片受体 (?-OR) 正变构调节剂。BMS-986122 显示正构激动剂介导的 β-抑制蛋白募集、腺苷酸环化酶抑制和 G 蛋白活化的增强作用。BMS-986122 增强 DAMGO 介导的 [³⁵S]GTPγS 在小鼠脑膜中的结合。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

In Vitro: BMS-986122 increases β-arrestin recruitment stimulated by endomorphin 1 (EC₅₀=3 μM) in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors.BMS-986122 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 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes and appears to be, at least in part, a positive affinity modulator of the μ-opioid receptor for DAMGO binding.
BMS-986122 enhances the ability of the endogenous opioid Methionine-enkephalin (Met-Enk) to stimulate G protein activity in mouse brain homogenates without activity on its own and to enhance G protein activation to a greater extent than β-arrestin recruitment in CHO cells expressing human mu-opioid receptors. BMS-986122 increases the potency of Met-Enk to inhibit GABA release in the periaqueductal gray, an important site for antinociception.
BMS-986122 is selective for ?-OR and has no detectable activity at the closely related δ-OR. BMS-986122 is a silent allosteric modulator at δ-OR and κ-OR.

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