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部分苯二氮䓬受体激动剂PK 8165对胆囊收缩素诱导的海马锥体神经元激活的影响:大鼠微离子电泳研究

Effects of PK 8165, a partial benzodiazepine receptor agonist, on cholecystokinin-induced activation of hippocampal pyramidal neurons: a microiontophoretic study in the rat.

作者信息

Bradwejn J, De Montigny C

出版信息

Eur J Pharmacol. 1985 Jun 19;112(3):415-8. doi: 10.1016/0014-2999(85)90790-3.

Abstract

Benzodiazepines (BZD) have been reported to suppress cholecystokinin-8S (CCK-8S)-induced activation. PK 8165, a ligand of BZD receptors, is an anxiolytic devoid of sedative and anticonvulsant effects. PK 8165, applied microiontophoretically or administered i.v. at low doses, suppressed CCK-8S-induced activation of hippocampal pyramidal neurons, whereas, at high doses it antagonized the effect of microiontophoretic applications of flurazepam. These results indicate that PK 8165 acts as a mixed agonist-antagonist at BZD receptors and suggest that the suppression of CCK-8S-induced activation by BZD might be related to their anxiolytic property rather than to their sedative or anticonvulsant activity.

摘要

据报道,苯二氮䓬类药物(BZD)可抑制胆囊收缩素-8S(CCK-8S)诱导的激活。PK 8165是一种BZD受体配体,是一种无镇静和抗惊厥作用的抗焦虑药。以微量离子透入法应用或静脉注射低剂量的PK 8165,可抑制CCK-8S诱导的海马锥体神经元激活,而高剂量时它可拮抗微量离子透入法应用氟西泮的作用。这些结果表明,PK 8165在BZD受体上起混合激动剂-拮抗剂的作用,并提示BZD对CCK-8S诱导激活的抑制作用可能与其抗焦虑特性有关,而非与其镇静或抗惊厥活性有关。

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