Open channel block and open channel destabilization:: contrasting effects of phenol, TEA+ and local anaesthetics on Kv1.1 K+ channels

被引：9

作者：

Elliott, AA ^{[1
]}

Harrold, JA ^{[1
]}

Newman, JP ^{[1
]}

Elliott, JR ^{[1
]}

机构：

[1] Univ Dundee, Dept Anat & Physiol, Dundee DD1 4HN, Scotland

来源：

TOXICOLOGY LETTERS | 1998年 / 101卷

基金：

英国惠康基金;

关键词：

K+ channels; TEA(+); phenol; channel inhibition;

D O I：

10.1016/S0378-4274(98)00196-9

中图分类号：

R99 [毒物学（毒理学）];

学科分类号：

100405 ;

摘要：

:1(0)(1) Voltage-gated K+ channels are inhibited by a variety of clinical and experimental drugs. (2) Complex changes in channel gating suggest mechanisms in which drug affinity depends on channel state. (3) Here, we use the effects of external TEA(+), two local anaesthetics (lidocaine and bupivacaine), and phenol on rat brain Kvl.l K+ channels expressed in Xenopus oocytes to illustrate three mechanisms. (4) The open state has the highest affinity in the local anaesthetic model but the lowest in the phenol model, and while local anaesthetics simply block the open channel, phenol can produce a conducting but destabilized open state. (5) All states have equal affinity for external TEA(+). (C) 1998 Elsevier Science Ireland Ltd. All rights reserved.

引用

页码：277 / 285

页数：9

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