γ-氨基丁酸（GABA）反应的多种拮抗机制。
Multiple mechanisms of antagonism of gamma-aminobutyric acid (GABA) responses.
作者信息
Akaike N, Yakushiji T, Tokutomi N, Carpenter D O
出版信息
Cell Mol Neurobiol. 1987 Mar;7(1):97-103. doi: 10.1007/BF00734993.
Abstract
Gamma-aminobutyric acid (GABA) is one of the most important neurotransmitters in the brain. In an effort to understand the operation of the GABA receptor-ionophore complex, the antagonism of GABA responses by four substances was studied in bullfrog dorsal root ganglion cells by concentration-clamp and internal-perfusion techniques. Two antagonists (bicuculline and Zn2+) were competitive; two (picrotoxin and penicillin) were noncompetitive. However, significant changes in the kinetics of activation and inactivation were produced by the antagonists, including those that were competitive. The causes of these changes may be important clues to the structure and operation of the GABA receptor-ionophore complex.
摘要
γ-氨基丁酸（GABA）是大脑中最重要的神经递质之一。为了了解GABA受体-离子载体复合物的运作，通过浓度钳制和内部灌注技术，在牛蛙背根神经节细胞中研究了四种物质对GABA反应的拮抗作用。两种拮抗剂（荷包牡丹碱和Zn2+）具有竞争性；两种（印防己毒素和青霉素）是非竞争性的。然而，拮抗剂会使激活和失活的动力学发生显著变化，包括那些具有竞争性的拮抗剂。这些变化的原因可能是GABA受体-离子载体复合物结构和运作的重要线索。
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