Abstract：
The nine G protein-coupled adrenoceptor subtypes are where the endogenous catecholamines adrenaline and noradrenaline interact with cells. Since they are important therapeutic targets, over a century of effort has been put into developing drugs that modify their activity. This chapter provides an outline of how we have arrived at current knowledge of the receptors, their physiological roles and the methods used to develop ligands. Initial studies in vivo and in vitro with isolated organs and tissues progressed to cell-based techniques and the use of cloned adrenoceptor subtypes together with high-throughput assays that allow close examination of receptors and their signalling pathways. The crystal structures of many of the adrenoceptor subtypes have now been determined opening up new possibilities for drug development.
摘要：
9种G蛋白偶联的肾上腺素受体亚型是内源性儿茶酚胺肾上腺素和去甲肾上腺素与细胞相互作用的地方。因为它们是重要的治疗靶点，一个多世纪以来，人们一直致力于开发改变其活性的药物。本章概述了我们如何获得受体的当前知识，它们的生理作用和用于开发配体的方法。对分离的器官和组织进行体内和体外的初步研究发展到基于细胞的技术和克隆的肾上腺素受体亚型的使用以及允许密切检查受体及其信号传导途径的高通量测定。现在已经确定了许多肾上腺素受体亚型的晶体结构，为药物开发开辟了新的可能性。
