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新型中枢性肌肉松弛剂阿夫喹酮对大鼠DRL反应和CER的影响(作者译)

[Effects of afloqualone, a new centrally acting muscle relaxant, on DRL response and CER in rats (author's transl)].

作者信息

Yamamura M, Ochiai T, Ishida R

出版信息

Nihon Yakurigaku Zasshi. 1981 Oct;78(4):381-92.

PMID:6120127
Abstract

In gross-behavioral observations, chlordiazepoxide, diazepam, meprobamate, and pentobarbital-Na produced excitatory behavior at 5 and 10, 1 and 2, 100 and 200, and 10 and 20 mg/kg p.o., respectively whereas afloqualone produced no excitatory behavior at doses up to 20 mg/kg p.o., these doses induce muscle relaxation and motor depression. Afloqualone depressed DRL response at 10 and 20 mg/kg p.o. Similar effects were seen with chlorpromazine (5, 10, 20 mg/kg p.o.). Chlordiazepoxide, meprobamate, and pentobarbital-Na facilitated DRL response at doses producing excitatory behavior. Methamphetamine (0.5, 1, 2 mg/kg p.o.) facilitated the response, dose-dependently. In CER, chlordiazepoxide (5, 10, 20 mg/kg p.o.), diazepam (1, 2, 5 mg/kg p.o.), and meprobamate (50, 100, 200 mg/kg p.o.) dose-dependently increased the response during the alarm period, regardless of the response during the safe period. Pentobarbital-Na (5, 10, 20 mg/kg p.o.) had much the same effect. Afloqualone slightly increased the response during the alarm period in one out of 3 rats at 5, 10, and 20 mg/kg p.o., respectively. Chlorpromazine and methamphetamine had no influence on the response during the alarm period at doses up to 20 and 2 mg/kg p.o., respectively. These results suggest that the pharmacological properties of afloqualone, as related to behavior differ from those of anti-anxiety drugs, hypnotics, and stimulants.

摘要

在总体行为观察中,氯氮卓、地西泮、甲丙氨酯和戊巴比妥钠分别在口服剂量为5和10mg/kg、1和2mg/kg、100和200mg/kg以及10和20mg/kg时产生兴奋行为,而阿氟喹酮在口服剂量高达20mg/kg时未产生兴奋行为,这些剂量会引起肌肉松弛和运动抑制。阿氟喹酮在口服剂量为10和20mg/kg时抑制了DRL反应。氯丙嗪(口服剂量为5、10、20mg/kg)也有类似效果。氯氮卓、甲丙氨酯和戊巴比妥钠在产生兴奋行为的剂量下促进了DRL反应。甲基苯丙胺(口服剂量为0.5、1、2mg/kg)剂量依赖性地促进了反应。在CER中,氯氮卓(口服剂量为5、10、20mg/kg)、地西泮(口服剂量为1、2、5mg/kg)和甲丙氨酯(口服剂量为50、100、200mg/kg)剂量依赖性地增加了警报期的反应,无论安全期的反应如何。戊巴比妥钠(口服剂量为5、10、20mg/kg)也有大致相同的效果。阿氟喹酮在口服剂量分别为5、10和20mg/kg时,在3只大鼠中有1只在警报期略微增加了反应。氯丙嗪和甲基苯丙胺在口服剂量分别高达20和2mg/kg时对警报期的反应没有影响。这些结果表明,阿氟喹酮与行为相关的药理特性不同于抗焦虑药物、催眠药和兴奋剂。

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