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1,4 - 二氢吡啶激活剂与拮抗剂:结构与功能差异

1,4-Dihydropyridine activators and antagonists: structural and functional distinctions.

作者信息

Triggle D J, Rampe D

出版信息

Trends Pharmacol Sci. 1989 Dec;10(12):507-11. doi: 10.1016/0165-6147(89)90051-5.

DOI:10.1016/0165-6147(89)90051-5
PMID:2694544
Abstract

The dihydropyridine series of drugs contains both potent antagonists and potent activators of Ca2+ channels. The structural differences between antagonists and activators are small and, indeed, activators can behave as antagonists at high levels of membrane depolarization. Here, David Triggle and David Rampe describe recent insights into the factors--including structure of the drug and activation state of the channel--that influence the behavior of these drugs, and discuss models that have been proposed to describe their mechanism of action.

摘要

二氢吡啶类药物既包含强效的钙通道拮抗剂,也包含强效的钙通道激活剂。拮抗剂和激活剂之间的结构差异很小,实际上,在膜高度去极化时,激活剂可表现出拮抗剂的作用。在此,大卫·特里格尔和大卫·兰普描述了近期对影响这些药物作用的因素(包括药物结构和通道激活状态)的见解,并讨论了已提出的描述其作用机制的模型。

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