丁螺环酮对人类志愿者热感觉和痛阈的影响。

Goran Pavlaković, Julija Tigges, Thomas A Crozier
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引用次数: 26

摘要

背景:丁螺环酮是部分5-HT1A受体激动剂。动物研究表明,调节5-HT1A受体的5-羟色胺能传递可以诱导急性疼痛模型的镇痛。然而,到目前为止,还没有关于血清素受体激动剂对人类疼痛感知的影响的研究发表。方法:采用前瞻性、随机、双盲、双假、安慰剂对照研究,观察丁螺环酮(30 mg p.o)对12名女性志愿者(26±2岁)热感觉和疼痛阈值的影响,吗啡(10 mg静脉注射)为阳性对照。结果:吗啡在60分钟显著提高热痛检测阈值(DeltaT:安慰剂1.0℃和1.3℃,p < 0.05)。丁螺环酮在60分钟内对6名参与者产生轻度镇静作用,但对任何测量参数都没有影响。结论:丁螺环酮在最大推荐剂量下对热痛无显著影响。然而,由于它只是5-HT1A受体的部分激动剂,并且还作用于其他受体类型,因此本研究的阴性结果并不排除更特异性的5-HT1A受体激动剂可能具有镇痛作用。
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Effect of buspirone on thermal sensory and pain thresholds in human volunteers.

Background: Buspirone is a partial 5-HT1A receptor agonist. Animal studies have shown that modulation of serotoninergic transmission at the 5-HT1A receptor can induce analgesia in acute pain models. However, no studies have been published so far on the effects of serotonin receptor agonists on pain perception in humans.

Methods: The effects of buspirone (30 mg p.o.) on thermal sensory and pain thresholds were investigated in twelve female volunteers (26 +/- 2 yrs) in a prospective, randomized, double-blind, double-dummy, placebo-controlled study with morphine (10 mg i.v.) as positive control.

Results: Morphine significantly increased the heat pain detection threshold (DeltaT: placebo 1.0 degrees C and 1.3 degrees C, p < 0.05) at 60 minutes. Buspirone caused mild sedation in six participants at 60 minutes, but was without effect on any of the measured parameters.

Conclusion: Buspirone in the maximal recommended dose was without significant effect on thermal pain. However, as it is only a partial agonist at the 5-HT1A receptor and also acts on other receptor types, the negative results of the present study do not rule out a possible analgesic effect of more specific 5-HT1A receptor agonists.

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