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外周苯二氮䓬受体特异性拮抗剂PK 11 195对长期暴露于地西泮的大鼠体重的影响。

The effect of PK 11 195, a specific antagonist of the peripheral benzodiazepine receptors, on body weight in rats chronically exposed to diazepam.

作者信息

Jing X, Wala E P, Sloan J W

机构信息

Department of Anesthesiology, University of Kentucky, College of Medicine, Lexington, KY 40503-0293, USA.

出版信息

Pharmacol Res. 2000 Sep;42(3):227-34. doi: 10.1006/phrs.2000.0686.

DOI:10.1006/phrs.2000.0686
PMID:10945928
Abstract

This study was undertaken to evaluate the effect of acute and repeated (daily and weekly) intravenous (IV) administration of PK 11 195 (PK; 10 mg kg(-1)) on body weight (BW) in Sprague-Dawley male and female rats exposed for 4-8 weeks to diazepam (DZ) slowly released from Silastic capsules (120 and 90 mg/capsule/week for males and females, respectively). Rats implanted with empty capsules served as controls. Both acute and repeated (daily and weekly) administration of PK inhibited BW gain to a greater extent in male than in female rats that received identical treatment. There was no difference in PK effect between DZ-treated and control rats. Furthermore, regardless of treatment or gender, PK-induced inhibition of BW gain lessened during repeated administration of PK. The present data indicate that PK-induced inhibition of BW gain is related to gender rather than to chronic DZ treatment.

摘要

本研究旨在评估对4至8周内从硅橡胶胶囊(分别为雄性和雌性每周120和90毫克/胶囊)缓慢释放地西泮(DZ)的Sprague-Dawley雄性和雌性大鼠,急性和重复(每日和每周)静脉注射(IV)PK 11 195(PK;10毫克/千克)对体重(BW)的影响。植入空胶囊的大鼠作为对照。在接受相同治疗的雄性和雌性大鼠中,急性和重复(每日和每周)给予PK均比雌性大鼠更大程度地抑制体重增加。接受DZ治疗的大鼠和对照大鼠之间PK效应没有差异。此外,无论治疗或性别如何,在重复给予PK期间,PK诱导的体重增加抑制作用都会减轻。目前的数据表明,PK诱导的体重增加抑制与性别有关,而与慢性DZ治疗无关。

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