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阿扑吗啡对大鼠疼痛的相反作用。剂量反应曲线评估。

Opposing effects of apomorphine on pain in rats. Evaluation of the dose-response curve.

作者信息

Paalzow G H, Paalzow L K

出版信息

Eur J Pharmacol. 1983 Mar 18;88(1):27-35. doi: 10.1016/0014-2999(83)90388-6.

Abstract

The effect of apomorphine on a supraspinally mediated response to pain was studied after subcutaneous administration of 10 different doses (25 micrograms/kg up to 10 mg/kg). Depending on the dose given, apomorphine was found to induce opposing effects on pain, so that low doses, 25-100 micrograms/kg, dose-dependently increased the sensitivity to pain. This effect then gradually declined in potency with increasing doses and high doses induced antinociception. The data therefore suggest that the net effect recorded involves the sum of responses from at least two functional systems. Using the Hill equation and the digital computer program NONLIN, we have dissociated the observed effect into two components, each having its particular dose-response characteristics: low doses having an ED50 value of 36 micrograms/kg produced hyperreactivity to pain, and high doses having an ED50 of 465 micrograms/kg (in the absence of hyperalgesia) induced antinociception.

摘要

皮下注射10种不同剂量(25微克/千克至10毫克/千克)的阿扑吗啡后,研究了其对脊髓上介导的疼痛反应的影响。根据所给剂量,发现阿扑吗啡对疼痛产生相反的作用,即低剂量(25 - 100微克/千克)剂量依赖性地增加对疼痛的敏感性。随着剂量增加,这种作用的效力逐渐下降,高剂量则诱导抗伤害感受。因此,数据表明所记录的净效应涉及至少两个功能系统的反应总和。使用希尔方程和数字计算机程序NONLIN,我们将观察到的效应分解为两个成分,每个成分都有其特定的剂量 - 反应特征:低剂量(ED50值为36微克/千克)产生对疼痛的高反应性,高剂量(ED50为465微克/千克,无痛觉过敏)诱导抗伤害感受。

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