组胺受体3拮抗剂对神经病理性疼痛的治疗作用

Effect of histamine receptor 3 antagonists on neuropathic pain

目的探讨脑室内注射组胺受体3拮抗剂对神经病理性疼痛大鼠的治疗作用。方法选择左侧坐骨神经部分结扎致神经病理性疼痛大鼠30只,脑室内给药。大鼠随机分为脑室内对照组、脑室内组胺受体3(H3R)拮抗剂-thioperamide组(50μg)、脑室内H3R激动剂R-α-甲基组胺组(RAMH,4μg),评价注药后痛阈的改变。结果与对照组相比,脑室内给予thioperamide 10min后起效,持续至100min,能显著提高大鼠对机械性刺激的痛阈(P﹤0.01),缓解疼痛。同时予RAMH30～50min后引起疼痛且能加重痛觉过敏(P﹤0.05)。结论神经病理性疼痛时,采用组胺受体3拮抗剂脑室内给药能提高痛阈,可以缓解疼痛。

Objective To investigate the effect of histamine receptor 3 agonist and antagonist on mechanical pain threshold of neuropathic pain rat and to find out whether there is an antinociceptive effect of histamine receptor 3 ligands on neuropathic pain. Methods In rats, the sciatic nerve was partially ligated and neuropathic pain were induced. Two weeks later, histamine receptor 3 agonist-R-α-methylhistamine and antagonists-thioperamide, and saline were respectively injected intracerebroventricularly into neuropathic pain rats and the effect of these medicine on mechanical pain threshold were measured. Results There was signifigant increase of the pain threshold in the thioperamide group, on the other hand, R-α-methylhistamine significantly decreased the pain threshold compared with the control group, which aggravated the hyperpalgesia in rats with neuropathic pain. Conclusions Intracerebroventricular administration of histamine receptor 3 antagonist can induce antinociception in rats with neumpathic pain.