Pharmacological Profiles of Oligomerized μ-Opioid Receptors.
Pharmacological Profiles of Oligomerized μ-Opioid Receptors.
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作者：
Lee CW;Ho IK
阿片类药物是广泛使用的止痛药，具有多种副作用和潜在的并发症。它们通过 G 蛋白-蛋白偶联受体产生镇痛作用：μ-、δ-、κ-阿片类药物和类阿片受体 1 受体。针对寡聚阿片受体的二价配体可能是开发没有不良副作用的镇痛药以及为阿片类药物成瘾者提供有效治疗的关键。在这篇综述中，我们将更新μ-阿片类药物对同源或异源寡聚μ-阿片受体的生物效应，并讨论二价配体发挥有益作用的潜在机制，包括腺苷酸环化酶调节和受体介导的信号通路。
Opioids are widely prescribed pain relievers with multiple side effects and potential complications. They produce analgesia via G-protein-protein coupled receptors: μ-, δ-, κ-opioid and opioid receptor-like 1 receptors. Bivalent ligands targeted to the oligomerized opioid receptors might be the key to developing analgesics without undesired side effects and obtaining effective treatment for opioid addicts. In this review we will update the biological effects of μ-opioids on homo- or hetero-oligomerized μ-opioid receptor and discuss potential mechanisms through which bivalent ligands exert beneficial effects, including adenylate cyclase regulation and receptor-mediated signaling pathways.