Fukuda K
Department of Anesthesia, Kyoto University Hospital.
Masui. 1996 Sep;45(9):1060-66.
Pharmacological actions of opioid analgesics are mediated by the mu-, delta- and kappa-opioid receptors in the nervous system. To understand the molecular basis of the opioid receptor functions, experiments using molecular biological methods have been performed. Amino acid sequences elucidated by cDNA cloning revealed that the opioid receptor possesses characteristic structural features of the G-protein-coupled receptor family, including the presence of seven transmembrane segments. Furthermore, molecular mechanism for the ligand selectivity of the mu- and delta-opioid receptors was investigated by analyzing chimeric receptors between the mu- and delta-receptors and mutant receptors with one amino acid replacement.
阿片类镇痛药的药理作用是由神经系统中的μ-、δ-和κ-阿片受体介导的。为了了解阿片受体功能的分子基础,已经进行了使用分子生物学方法的实验。通过cDNA克隆阐明的氨基酸序列显示,阿片受体具有G蛋白偶联受体家族的特征性结构特征,包括存在七个跨膜区段。此外,通过分析μ-和δ-受体之间的嵌合受体以及具有一个氨基酸替换的突变受体,研究了μ-和δ-阿片受体配体选择性的分子机制。