Rosland J H, Hunskaar S, Hole K
Department of Physiology, University of Bergen, Norway.
Pharmacol Toxicol. 1987 Aug;61(2):111-5. doi: 10.1111/j.1600-0773.1987.tb01786.x.
The antinociceptive properties of diazepam were evaluated in mice, using four different pain tests and different doses of the drug (0.2, 0.5, 1.0 and 2.0 mg/kg). In the tail flick test and the increasing temperature hot plate test there were no effects. In the formalin test reduced licking was observed for the highest dose of diazepam. However, this dose also induced clear sedation possibly causing the reduced licking response. In the constant temperature hot plate test a hyperalgesia was found for all doses tested. This hyperalgesia was not observed in animals adapted to the test apparatus, suggesting that the "hyperalgesic" effect of diazepam may be due to reduced stress analgesia. The serum concentrations of the drug were comparable to therapeutic levels in humans. It was concluded that the sedative and anxiolytic effects of diazepam may influence the results of nociceptive tests, but the drug has probably no effect on nociception in itself.
使用四种不同的疼痛测试方法和不同剂量(0.2、0.5、1.0和2.0毫克/千克)的地西泮对小鼠的抗伤害感受特性进行了评估。在甩尾试验和渐增温度热板试验中未观察到效果。在福尔马林试验中,观察到最高剂量的地西泮使舔舐行为减少。然而,该剂量也引起了明显的镇静作用,这可能导致舔舐反应减少。在恒温热板试验中,所有测试剂量均发现有痛觉过敏现象。在适应测试装置的动物中未观察到这种痛觉过敏现象,这表明地西泮的“痛觉过敏”效应可能是由于应激镇痛作用减弱所致。该药物的血清浓度与人类治疗水平相当。得出的结论是,地西泮的镇静和抗焦虑作用可能会影响伤害感受测试的结果,但该药物本身可能对痛觉感受没有影响。