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鞘内注射氟马西尼和PK 11195可使自由活动的地西泮依赖大鼠出现戒断综合征。

Intrathecally administered flumazenil and PK 11195 precipitate abstinence syndrome in freely moving diazepam dependent rats.

作者信息

Wala E P, Sloan J W, Jing X, Holtman P H

机构信息

University of Kentucky, Department of Anesthesiology, Lexington, USA.

出版信息

Drug Alcohol Depend. 1996 Dec 11;43(3):169-77. doi: 10.1016/s0376-8716(96)01307-5.

DOI:10.1016/s0376-8716(96)01307-5
PMID:9023073
Abstract

The central and peripheral benzodiazepine (BZ) receptor antagonists, flumazenil (FLU) and PK 11195 (PK), administered intrathecally (IT) to diazepam (DZ)-dependent rats produced a precipitated abstinence syndrome. The scores for abstinence increased with increasing dose of FLU but not with increasing dose of PK. Twitches and jerks increased with increased doses of both. Head and body tremors were produced by FLU, but not by PK. Neither FLU nor PK precipitated abstinence in controls. In DZ-dependent rats IT administered FLU and PK did not significantly change the spectral content and the total power of the EEG. The data indicate that an abstinence syndrome is precipitated at the spinal level in DZ-dependent rats and that both central and peripheral BZ receptors are involved.

摘要

向依赖地西泮(DZ)的大鼠鞘内注射中枢和外周苯二氮䓬(BZ)受体拮抗剂氟马西尼(FLU)和PK 11195(PK),可引发戒断综合征。戒断评分随FLU剂量增加而升高,但不随PK剂量增加而升高。抽搐和痉挛均随两种药物剂量增加而增多。FLU可引发头部和身体震颤,而PK则不会。在对照组中,FLU和PK均未引发戒断反应。在依赖DZ的大鼠中,鞘内注射FLU和PK对脑电图的频谱内容和总功率均无显著影响。数据表明,在依赖DZ的大鼠中,脊髓水平可引发戒断综合征,且中枢和外周BZ受体均参与其中。

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