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小鼠中的巴氯芬镇痛作用:一种由GABAB介导的反应。

Baclofen analgesia in mice: a GABAB-mediated response.

作者信息

Aley K O, Kulkarni S K

机构信息

Department of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

Methods Find Exp Clin Pharmacol. 1991 Dec;13(10):681-6.

PMID:1663195
Abstract

The effect of baclofen, a GABAB agonist, has been studied in three antinociceptive tests (tail flick latency, hot plate method and acetic acid-induced writhing) in mice. In all three models, baclofen was found to elicit a dose-dependent antinociceptive effect. The observed antinociceptive effect was stereospecific, as the levo isomer of baclofen was found to be more potent than the racemic mixture. Baclofen also potentiated morphine analgesia. The antinociceptive effect of baclofen was reversed by both CGP 35348, a GABAB antagonist, and naloxone, an opioid antagonist, but not by bicuculline or picrotoxin, GABAA antagonists. However, in acetic acid-induced writhing, naloxone failed to reverse baclofen analgesia. The data suggest that the antinociceptive effect of baclofen is GABAB receptor-mediated and that there may be a GABAergic and opiate/or non-opiate interaction in eliciting the analgesic effect.

摘要

已在小鼠的三项抗伤害感受试验(甩尾潜伏期、热板法和乙酸诱导扭体)中研究了GABAB激动剂巴氯芬的作用。在所有这三种模型中,发现巴氯芬可引发剂量依赖性抗伤害感受作用。观察到的抗伤害感受作用具有立体特异性,因为发现巴氯芬的左旋异构体比消旋混合物更有效。巴氯芬还增强了吗啡镇痛作用。巴氯芬的抗伤害感受作用被GABAB拮抗剂CGP 35348和阿片类拮抗剂纳洛酮逆转,但未被GABAA拮抗剂荷包牡丹碱或苦味毒逆转。然而,在乙酸诱导扭体试验中,纳洛酮未能逆转巴氯芬的镇痛作用。数据表明,巴氯芬的抗伤害感受作用是由GABAB受体介导的,并且在引发镇痛作用方面可能存在GABA能与阿片类/或非阿片类相互作用。

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