Receptors for γ‐aminobutyric acid and voltage‐dependent chloride channels as targets for drugs and toxicants 1
Receptors for γ‐aminobutyric acid and voltage‐dependent chloride channels as targets for drugs and toxicants 1
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γ-氨基丁酸和电压依赖性氯离子通道受体作为药物和毒物的靶标 1
DOI：
--
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发表时间：
1987
期刊：
影响因子：
--
通讯作者：
M. Eldefrawi
中科院分区：
文献类型：
--
作者：
A. Eldefrawi;M. Eldefrawi
氯离子（Cl−）通道蛋白的功能是调节Cl−跨膜转运。有两种主要的Cl−通道：1）通过结合递质（如γ-氨基丁酸（GABA）、甘氨酸或谷氨酸）激活的通道，因此是受体; 2）通过膜去极化或钙激活的通道。GABA受体有两种：GABAA是脊椎动物大脑中主要的抑制性受体，也是控制Cl−通道的一种; GABAB受体，被认为是调节由其他受体刺激的cAMP产生的受体。除了结合GABA外，这两种GABA受体在药物特异性上完全不同。然而，GABAA受体、甘氨酸受体和电压依赖性Cl−通道之间有许多相似之处。两种受体和Cl−通道结合阿维菌素，而荷包牡丹碱仅结合哺乳动物GABAA和甘氨酸受体，不结合昆虫脑GABAA受体。巴比妥酸盐与GABAA和电压依赖性Cl−通道结合，可能直接激活它们。苯二氮卓类药物可增强甘氨酸和GABAA受体。几种杀虫剂作用于GABAA受体和电压依赖性Cl−通道。这表明GABAA受体是毒杀芬和环二烯类杀虫剂作用的主要靶点，但对林螨和II型拟除虫菊酯是次要靶点。另一方面，Cl−通道可能是阿维菌素和林螨素的主要靶点，但对环二烯来说是次要靶点。某些药物特异性和Cl−通道操作的相似性表明GABAA和甘氨酸受体亚基与电压依赖性Cl−通道之间存在一定程度的同源性。Eldefrawi，A. T.; Eldefrawi，M. E.作为药物和毒物靶点的γ-氨基丁酸和电压依赖性氯离子通道受体。FASEB J. 1：262 - 271; 1987.
The function of chloride (Cl−) channel proteins is to regulate the transport of Cl− across membranes. There are two major kinds of Cl− channels: 1) those activated by binding of a transmitter such as γ‐aminobutyric acid (GABA), glycine, or glutamate, and thus are receptors; and 2) those activated by membrane depolarization or by calcium. There are two kinds of GABA receptors: GABAA is the major inhibitory receptor of vertebrate brain and the one that operates a Cl− channel, and the GABAB receptor, which is proposed to regulate cAMP production that is stimulated by other receptors. Except for binding of GABA, these two GABA receptors differ completely in their drug specificities. However, there are many similarities among the GABAA receptor, the glycine receptor, and the voltage‐dependent Cl− channel. The two receptors and Cl− channels bind avermectin, whereas bicuculline binds only to mammalian GABAA and glycine receptors, not to the insect brain GABAA receptor. Barbiturates bind to GABAA and voltage‐dependent Cl− channels, possibly directly activating them. Benzodiazepines potentiate both the glycine and GABAA receptors. Several insecticides act on the GABAA receptor and voltage‐dependent Cl− channel. It is suggested that the GABAA receptor is the primary target for the action of toxaphene and cyclodiene insecticides but a secondary target for lindane and type II pyrethroids. On the other hand, the Cl− channel may be a primary target for avermectin and lindane but a secondary one for cyclodienes. The similarity in certain drug specificities and the operation of Cl− channels suggest a degree of homology between the subunits of GABAA and glycine receptors and the voltage‐dependent Cl− channels.—Eldefrawi, A. T.; Eldefrawi, M. E. Receptors for γ‐aminobutyric acid and voltage‐dependent chloride channels as targets for drugs and toxicants. FASEB J. 1: 262‐271; 1987.
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GABA 受体通道药物与鱼雷电器官中假定的电压依赖性氯离子通道的结合。
影响因子：
5.8
作者：
Abalis,IM;Eldefrawi,ME;Eldefrawi,AT
通讯作者：
Eldefrawi,AT
DOI：
10.1080/03601238309372355
发表时间：
1983
期刊：
Journal of environmental science and health. Part. B, Pesticides, food contaminants, and agricultural wastes
影响因子：
--
作者：
F. Matsumura;S. M. Ghiasuddin
通讯作者：
F. Matsumura;S. M. Ghiasuddin
DOI：
--
发表时间：
1986-11
期刊：
Federation proceedings
影响因子：
--
作者：
R. Frizzell;D. Halm;G. Rechkemmer;R. Shoemaker
通讯作者：
R. Frizzell;D. Halm;G. Rechkemmer;R. Shoemaker
阿维菌素 B1a 对大鼠脑中 γ-氨基丁酸 A 受体和氯离子通道的作用。
DOI：
10.1002/jbt.2570010108
发表时间：
1986
期刊：
Journal of biochemical toxicology
影响因子：
--
作者：
Abalis,IM;Eldefrawi,AT;Eldefrawi,ME
通讯作者：
Eldefrawi,ME
双环磷酯和一些多氯环烷烃和拟除虫菊酯杀虫剂与脑特异性叔丁基二环硫代磷酸酯受体相互作用的结构-活性相关性。
影响因子：
10.4
作者：
Casida,JE;Lawrence,LJ
通讯作者：
Lawrence,LJ