肾上腺素能受体基因敲除小鼠：9种受体亚型的不同功能

Adrenergic receptor knockout mice: distinct functions of 9 receptor subtypes.

作者信息

Philipp Melanie, Hein Lutz

机构信息

Institute of Pharmacology and Toxicology, University of Würzburg, Versbacher Strasse 9, D-97078, Würzburg, Germany.

出版信息

Pharmacol Ther. 2004 Jan;101(1):65-74. doi: 10.1016/j.pharmthera.2003.10.004.

DOI:10.1016/j.pharmthera.2003.10.004

PMID:14729393

Abstract

The biological effects of epinephrine and norepinephrine are mediated via 9 different adrenergic receptor subtypes, which all belong to the superfamily of G protein-coupled receptors. Although pharmacological ligands for adrenergic receptors have an important place in medical therapy, the full therapeutic potential of the 9 adrenergic receptor subtypes has not been explored yet. To dissect the physiological relevance of adrenergic receptor subtype diversity, gene-targeted mouse models carrying deletions in these receptor genes ("knockout mice") have been generated. This review gives an overview of the phenotypes observed in mice deficient in adrenergic receptors and discusses the therapeutic relevance of subtype-specific drug therapy.

摘要

肾上腺素和去甲肾上腺素的生物学效应是通过9种不同的肾上腺素能受体亚型介导的，这些亚型均属于G蛋白偶联受体超家族。尽管肾上腺素能受体的药理学配体在医学治疗中占有重要地位，但9种肾上腺素能受体亚型的全部治疗潜力尚未得到充分探索。为了剖析肾上腺素能受体亚型多样性的生理相关性，已构建了在这些受体基因中携带缺失的基因靶向小鼠模型（“基因敲除小鼠”）。本综述概述了肾上腺素能受体缺陷小鼠中观察到的表型，并讨论了亚型特异性药物治疗的治疗相关性。