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苯二氮䓬拮抗剂CGS 8216可减少饥饿大鼠的食物摄入量。

CGS 8216, a benzodiazepine antagonist, reduces food intake in food-deprived rats.

作者信息

Bernard P S, Pastor G, Liebman J M

出版信息

Pharmacol Biochem Behav. 1986 Jun;24(6):1703-6. doi: 10.1016/0091-3057(86)90508-3.

Abstract

CGS 8216, a benzodiazepine receptor antagonist with weak inverse agonist properties, reduced food intake in food-deprived rats when administered orally or intraperitoneally at doses that antagonize diazepam. This effect was sustained when CGS 8216 was administered daily for five days, indicating no rapid tolerance to the anorectic effect. Ro 15-1788 did not reduce feeding when administered orally, and was active only at high intraperitoneal doses (54 and 100 mg/kg). CGS 9896, a close analog of CGS 8216 but a benzodiazepine partial agonist with anxiolytic properties, did not reduce food intake at doses as high as 100 mg/kg IP or PO. These results support prior suggestions that benzodiazepine receptors may modulate feeding behavior, and suggest that CGS 8216 may have appetite suppressant properties.

摘要

CGS 8216是一种具有弱反向激动剂特性的苯二氮䓬受体拮抗剂,当以拮抗地西泮的剂量口服或腹腔注射时,可减少饥饿大鼠的食物摄入量。当连续五天每天给予CGS 8216时,这种作用持续存在,表明对厌食作用没有快速耐受性。口服Ro 15 - 1788时不会减少进食,仅在高腹腔注射剂量(54和100 mg/kg)时才有活性。CGS 9896是CGS 8216的紧密类似物,但具有抗焦虑特性的苯二氮䓬部分激动剂,在高达100 mg/kg腹腔注射或口服剂量时不会减少食物摄入量。这些结果支持了先前关于苯二氮䓬受体可能调节进食行为的建议,并表明CGS 8216可能具有食欲抑制特性。

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