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硫酸孕烯醇酮通过降低通道开放频率来拮抗GABAA受体介导的电流。

Pregnenolone sulfate antagonizes GABAA receptor-mediated currents via a reduction of channel opening frequency.

作者信息

Mienville J M, Vicini S

机构信息

FIDIA-Georgetown Institute for the Neurosciences, Georgetown University Medical School, Washington 20007.

出版信息

Brain Res. 1989 Jun 5;489(1):190-4. doi: 10.1016/0006-8993(89)90024-3.

DOI:10.1016/0006-8993(89)90024-3
PMID:2472854
Abstract

Our previous study showed antagonism of GABAA receptor-mediated whole-cell currents by pregnenolone sulfate (PS). Here, the effects of PS, picrotoxin (PTX) and pentobarbital (PB) were tested on GABA-activated single Cl- channels recorded from membrane patches of rat cortical neurons in primary cultures. PS and PTX selectively decreased the opening frequency of the channels, while PB increased mean open time and burst duration without affecting opening frequency. It is suggested that PS and PTX may antagonize GABAA receptor function through the same mechanism and/or the same binding site.

摘要

我们之前的研究表明,硫酸孕烯醇酮(PS)可拮抗GABAA受体介导的全细胞电流。在此,我们测试了PS、印防己毒素(PTX)和戊巴比妥(PB)对原代培养大鼠皮质神经元膜片上记录的GABA激活的单Cl-通道的影响。PS和PTX选择性地降低了通道的开放频率,而PB增加了平均开放时间和爆发持续时间,且不影响开放频率。提示PS和PTX可能通过相同机制和/或相同结合位点拮抗GABAA受体功能。

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