Burnstock G
Department of Anatomy and Developmental Biology, University College London, UK.
Pharm Acta Helv. 1995 Mar;69(4):231-42. doi: 10.1016/0031-6865(94)00043-u.
It is hoped that this summary of the history and current status of purinoceptors will convince readers that receptors for purines are now established alongside other well-known extracellular messenger systems. These receptors are primitive, widespread and serve many different systems. Receptors of adenosine (P1-purinoceptors) are clearly different from receptors of ATP (P2-purinoceptors). As for other major transmitters such as acetylcholine, GABA, glutamate and 5-HT, receptors of two major families are activated by ATP, one (the P2X-purinoceptor family) mediates fast responses via ligand-gated ion channels, while the other (the P2Y-purinoceptor family) mediates slower responses via G-proteins (see Table 3). Subclasses of these two families have been suggested on the basis of recent molecular biology studies and the development of new selective agonists and antagonists (Abbracchio and Burnstock, 1994). It would indeed be helpful if the work on purinoceptors could be extended to studies of their chemical structure employing crystallography.
希望嘌呤受体的这段历史与现状总结能让读者相信,嘌呤受体如今已与其他知名的细胞外信使系统一同确立。这些受体原始且广泛存在,作用于许多不同的系统。腺苷受体(P1嘌呤受体)与ATP受体(P2嘌呤受体)明显不同。与其他主要递质如乙酰胆碱、GABA、谷氨酸和5-羟色胺一样,ATP可激活两个主要家族的受体,其中一个家族(P2X嘌呤受体家族)通过配体门控离子通道介导快速反应,另一个家族(P2Y嘌呤受体家族)则通过G蛋白介导较慢的反应(见表3)。基于近期分子生物学研究以及新型选择性激动剂和拮抗剂的开发,已提出这两个家族的亚类(阿布拉乔和伯恩斯托克,1994年)。如果能将嘌呤受体的研究扩展至利用晶体学对其化学结构进行研究的确会很有帮助。