Blake A D, Bot G, Tallent M, Law S F, Li S, Freeman J C, Reisine T
Department of Pharmacology, University of Pennsylvania, School of Medicine, Philadelphia 19104, USA.
Recept Channels. 1997;5(3-4):231-5.
Opioid actions are initiated at membrane receptors which couple to cellular effectors through G protein-mediated pathways. In the central nervous system opioids reduce neuronal activity through the inhibition of voltage-dependent Ca2+ channels, the activation of K+ channels and the inhibition of adenylyl cyclase. A significant clinical limitation to opioid therapy is the development of tolerance, a biological event that has been linked to agonist effects at the receptor level. Molecular studies on the consequences of opioid receptor regulation will provide a better understanding of the cellular mechanisms involved in the agonist-mediated events in tolerance development.
阿片类药物的作用始于膜受体，这些受体通过G蛋白介导的途径与细胞效应器偶联。在中枢神经系统中，阿片类药物通过抑制电压依赖性Ca2+通道、激活K+通道和抑制腺苷酸环化酶来降低神经元活性。阿片类药物治疗的一个重大临床局限性是耐受性的产生，这一生物学现象与受体水平的激动剂效应有关。对阿片受体调节后果的分子研究将有助于更好地理解耐受性发展过程中激动剂介导事件所涉及的细胞机制。
