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丁丙诺啡:其拮抗作用的剂量-反应曲线呈钟形。

Buprenorphine: bell-shaped dose-response curve for its antagonist effects.

作者信息

Lizasoain I, Leza J C, Lorenzo P

机构信息

Departamento de Farmacología, Facultad de Medicina, Universidad Complutense, Madrid, Spain.

出版信息

Gen Pharmacol. 1991;22(2):297-300. doi: 10.1016/0306-3623(91)90452-c.

Abstract
  1. Doses of buprenorphine (0.01, 0.1, 0.5, 1, 5, 10 and 50 mg/kg) were administered to determine buprenorphine's ability to precipitate abstinence symptoms in morphine-dependent mice. 2. When buprenorphine was administered in the fourth day of morphine addiction, the results demonstrate that the administration of the partial agonist opioid produce a bell-shaped dose-response curve. 3. The highest dose (50 mg/kg) was partially inactive while lower doses causing similar percentage than group treated with naloxone with respect to the appearance of the most of the symptoms of abstinence studied (diarrhoea, tremor, shaking-"wet dog shakes"-, jumping and weight loss). 4. Our findings demonstrate the bell-shaped response curve of the antagonist effects of buprenorphine.
摘要
  1. 给予不同剂量的丁丙诺啡(0.01、0.1、0.5、1、5、10和50毫克/千克),以确定丁丙诺啡在吗啡依赖小鼠中引发戒断症状的能力。2. 当在吗啡成瘾的第四天给予丁丙诺啡时,结果表明,给予部分激动剂阿片类药物会产生钟形剂量-反应曲线。3. 最高剂量(50毫克/千克)部分无活性,而较低剂量在研究的大多数戒断症状(腹泻、震颤、颤抖——“湿狗样抖动”——、跳跃和体重减轻)出现方面,与用纳洛酮治疗的组相比,引起的症状百分比相似。4. 我们的研究结果证明了丁丙诺啡拮抗作用的钟形反应曲线。

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