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脊髓培养物长期暴露于地西泮后苯二氮䓬结合的降低及地西泮对GABA介导的抑制作用的增强

Depression of benzodiazepine binding and diazepam potentiation of GABA-mediated inhibition after chronic exposure of spinal cord cultures to diazepam.

作者信息

Sher P K, Study R E, Mazzetta J, Barker J L, Nelson P G

出版信息

Brain Res. 1983 May 23;268(1):171-6. doi: 10.1016/0006-8993(83)90404-3.

DOI:10.1016/0006-8993(83)90404-3
PMID:6860959
Abstract

Cultures of fetal mouse spinal cord were exposed to 12.6 microM (3.6 micrograms/ml) diazepam for 7 days. After drug removal, benzodiazepine receptor binding was assayed on intact cells and intracellular recordings of diazepam effects on GABA-mediated inhibitory responses were obtained. The biochemical and electrophysiological data revealed significant and parallel reductions in both receptor binding and pharmacological action on GABA responses which did not return to control levels until 3-4 days after removal of diazepam. The results indicate that chronic exposure of spinal cord cultures to diazepam results in a reversible down-regulation of diazepam binding and function.

摘要

将胎鼠脊髓培养物暴露于12.6微摩尔(3.6微克/毫升)地西泮中7天。去除药物后,对完整细胞进行苯二氮䓬受体结合测定,并获得地西泮对γ-氨基丁酸(GABA)介导的抑制反应的细胞内记录。生化和电生理数据显示,受体结合以及对GABA反应的药理作用均显著且平行降低,直到去除地西泮3 - 4天后才恢复到对照水平。结果表明,脊髓培养物长期暴露于地西泮会导致地西泮结合和功能的可逆性下调。

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