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P2X嘌呤受体应如何进行药理学分类?

How should P2X purinoceptors be classified pharmacologically?

作者信息

Kennedy C, Leff P

机构信息

Department of Physiology and Pharmacology, University of Strathclyde, Royal College, UK.

出版信息

Trends Pharmacol Sci. 1995 May;16(5):168-74. doi: 10.1016/s0165-6147(00)89010-0.

Abstract

When ATP is released as a neurotransmitter from central and peripheral nerves it acts at P2X purinoceptors to produce postsynaptic depolarization and excitation. The P2X purinoceptor was originally classified on the basis of the relative agonist potencies of ATP and a number of its structural analogues. However, it is now clear that the potency of some agonists is greatly decreased by breakdown by ectonucleotidase enzymes, leading to an incorrect determination of agonist potency order. In this article, Charles Kennedy and Paul Leff discuss recent results that indicate that the established classification of P2X purinoceptors is no longer valid and needs redefinition.

摘要

当三磷酸腺苷(ATP)作为神经递质从中枢神经和外周神经释放时,它作用于P2X嘌呤受体,产生突触后去极化和兴奋。P2X嘌呤受体最初是根据ATP及其一些结构类似物的相对激动剂效力进行分类的。然而,现在很清楚的是,一些激动剂的效力会因外核苷酸酶的分解而大大降低,从而导致对激动剂效力顺序的错误判定。在本文中,查尔斯·肯尼迪和保罗·莱夫讨论了最近的研究结果,这些结果表明,已确立的P2X嘌呤受体分类不再有效,需要重新定义。

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