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巴氯芬[β-(4-氯苯基)-γ-氨基丁酸]的镇痛作用。

The analgesic action of baclofen [beta-(4-chlorophenyl)-gamma-aminobutyric acid].

作者信息

Levy R A, Proudfit H K

出版信息

J Pharmacol Exp Ther. 1977 Aug;202(2):437-45.

PMID:886473
Abstract

When administered to mice, baclofen induced dose-related antinocisponsive activity in the stretch, hot plate and tail-flick tests. Although high doses also impaired motor coordination, as measured by the rotating rod test, the following observations suggest that the pronounced antinocisponsive effect of higher doses did not reflect a reduced capacity to respond to perceived pain: motor impairment, having shorter onset of action, was fully developed before the appearance of any analgesic action; mice made completely tolerant to the motor effect were still analgesic; and other agents which severely impaired rotating rod performance did not necessarily show antinocisponsive activity in the hot plate test. The mechanism of action of baclofen is not similar to that of morphine since naloxone did not antagonize the analgesic effect of baclofen, and cross-tolerance between morphine- and baclofen-induced analgesia could not be demonstrated.

摘要

当给小鼠用药时,巴氯芬在伸展、热板和甩尾试验中诱导出剂量相关的抗伤害感受活性。尽管高剂量也会损害运动协调性(通过转棒试验测量),但以下观察结果表明,高剂量显著的抗伤害感受作用并非反映对感知疼痛的反应能力降低:运动损害起效时间较短,在任何镇痛作用出现之前就已充分显现;对运动效应产生完全耐受性的小鼠仍具有镇痛作用;而其他严重损害转棒表现的药物在热板试验中不一定表现出抗伤害感受活性。巴氯芬的作用机制与吗啡不同,因为纳洛酮不能拮抗巴氯芬的镇痛作用,且无法证明吗啡和巴氯芬诱导的镇痛之间存在交叉耐受性。

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