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Flunitrazepam rapidly reduces GABA(A) receptor subunit protein expression via a protein kinase C-dependent mechanism.氟硝西泮通过蛋白激酶C依赖性机制迅速降低GABA(A)受体亚基蛋白表达。
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2
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引用本文的文献

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Neurochemical and behavioral features in genetic absence epilepsy and in acutely induced absence seizures.遗传性失神癫痫和急性诱发失神发作的神经化学及行为特征。
ISRN Neurol. 2013 May 7;2013:875834. doi: 10.1155/2013/875834. Print 2013.
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The pentylenetetrazole allosteric component of the GABAA receptor plasticity.γ-氨基丁酸A受体可塑性的戊四氮变构成分。
Dokl Biol Sci. 2002 Sep-Oct;386:400-3. doi: 10.1023/a:1020745730228.
3
Rate of change of blood concentrations is a major determinant of the pharmacodynamics of midazolam in rats.血药浓度变化率是大鼠咪达唑仑药效学的主要决定因素。
Br J Pharmacol. 1999 May;127(1):227-35. doi: 10.1038/sj.bjp.0702499.

氟硝西泮通过蛋白激酶C依赖性机制迅速降低GABA(A)受体亚基蛋白表达。

Flunitrazepam rapidly reduces GABA(A) receptor subunit protein expression via a protein kinase C-dependent mechanism.

作者信息

Johnston J D, Price S A, Bristow D R

机构信息

Division of Neuroscience, School of Biological Sciences, University of Manchester.

出版信息

Br J Pharmacol. 1998 Aug;124(7):1338-40. doi: 10.1038/sj.bjp.0702012.

DOI:10.1038/sj.bjp.0702012
PMID:9723942
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1565552/
Abstract

Acute flunitrazepam (1 microM) exposure for 1 h reduced GABA(A) receptor alpha1 (22+/-4%, mean+/-s.e.mean) and beta2/3 (21+/-4%) subunit protein levels in cultured rat cerebellar granule cells. This rapid decrease in subunit proteins was completely prevented by bisindolymaleimide 1 (1 microM), an inhibitor of protein kinase C, but not by N-[2-((p-bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide (H-89, 4.8 microM), an inhibitor of protein kinases A and G. These results suggest the existence of a benzodiazepine-induced mechanism to rapidly alter GABA(A) receptor protein expression, that appears to be dependent on protein kinase C activity.

摘要

急性暴露于氟硝西泮（1微摩尔）1小时可降低培养的大鼠小脑颗粒细胞中GABA(A)受体α1亚基（22±4%，平均值±标准误平均值）和β2/3亚基（21±4%）的蛋白质水平。蛋白激酶C抑制剂双吲哚马来酰亚胺1（1微摩尔）可完全阻止亚基蛋白质的这种快速下降，但蛋白激酶A和G的抑制剂N-[2-((对溴肉桂基)氨基)乙基]-5-异喹啉磺酰胺（H-89，4.8微摩尔）则不能。这些结果表明存在一种苯二氮䓬诱导的机制来快速改变GABA(A)受体蛋白表达，这似乎依赖于蛋白激酶C的活性。