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苯二氮䓬受体与抗惊厥活性药理学相关性的证据。

Evidence for the pharmacological relevance of benzodiazepine receptors to anticonvulsant activity.

作者信息

Fisher T E, Johnson D D, Tuchek J M, Crawford R D

出版信息

Can J Physiol Pharmacol. 1985 Nov;63(11):1477-9. doi: 10.1139/y85-243.

Abstract

Each of a series of benzodiazepines was found to be effective in preventing convulsions evoked by intermittent photic stimulation of epileptic chickens. There was a high correlation between the anticonvulsant potencies (mean effective dosages) and the affinity of the agents for the putative benzodiazepine receptor as measured by displacement of [3H]diazepam from binding sites on chicken synaptosomal membranes. This correlation in a genetic model of epilepsy provides further evidence that benzodiazepines exert their anticonvulsant effects by interacting with the benzodiazepine receptor.

摘要

人们发现,一系列苯二氮䓬类药物中的每一种都能有效预防间歇性光刺激诱发的癫痫鸡惊厥。抗惊厥效力(平均有效剂量)与药物对假定的苯二氮䓬受体的亲和力之间存在高度相关性,该亲和力通过[³H]地西泮从鸡突触体膜结合位点的置换来测量。在癫痫的遗传模型中的这种相关性进一步证明,苯二氮䓬类药物通过与苯二氮䓬受体相互作用发挥其抗惊厥作用。

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