Fagura M S, Jarvis G E, Dougall I G, Leff P
Discovery BioScience, AstraZeneca R & D Charnwood, Bakewell Road, Leicestershire LE11 5RH, Loughborough, UK.
J Auton Nerv Syst. 2000 Jul 3;81(1-3):178-86. doi: 10.1016/s0165-1838(00)00136-3.
The pharmacological classification of P2 receptors owes its origin to the pioneering efforts of Geoff Burnstock and those who followed him, research that was conducted primarily in physiological experimental systems. Over recent years, the techniques of molecular biology have been increasingly applied in the study of P2 receptors while, at the same time, advances in their pharmacological analysis have been limited by a lack of potent and selective agonist or antagonist ligands. This has resulted in a classification scheme which is largely structural in nature, with relatively little contribution from pharmacology. Our endeavours in this area have been directed towards the discovery of ligands with which the pharmacological analysis and definition of P2 receptors could be advanced, the ultimate goal being the design of therapeutic agents. This article will describe some of our experiences in this challenging but rewarding area.
P2受体的药理学分类起源于 Geoff Burnstock 及其追随者的开创性工作，这些研究主要在生理实验系统中进行。近年来，分子生物学技术越来越多地应用于P2受体的研究，与此同时，由于缺乏强效和选择性激动剂或拮抗剂配体，其药理学分析进展有限。这导致了一种主要基于结构的分类方案，药理学的贡献相对较小。我们在这一领域的努力旨在发现能够推进P2受体药理学分析和定义的配体，最终目标是设计治疗药物。本文将描述我们在这个具有挑战性但回报丰厚的领域的一些经验。
