Jain N K, Kulkarni S K
Pharmacology Division, Panjab University, Chandigarh, India.
Indian J Exp Biol. 1998 Oct;36(10):973-9.
Antinociceptive effect of the antimigraine drug sumatriptan (5-HT1A agonist) was studied against acetic acid-induced writhing in mice. Sumatriptan produced the effect in a dose-dependent manner (1, 5, 10 and 20 mg/kg, s.c.). Naloxone (1 mg/kg i.p.) an opiate antagonist failed to reverse sumatriptan-induced antinociception. Cholinomimetic physostigmine (0.05 mg/kg, i.p.) potentiated and the muscarinic antagonist atropine (5 mg/kg, i.p.) blocked the antinociceptive effect of sumatriptan, respectively. The antinociceptive effect of sumatriptan was compared with an another 5-HT agonist (5-HT1A) buspirone which also produced antinociception. Like sumatriptan-analgesia, the buspirone response was also potentiated by physostigmine in atropine sensitive way. Further, buspirone potentiated the analgesic effect of sumatriptan. These observations suggest that 5-HT1A agonists produce antinociception possibly by modulating central cholinergic activity.
研究了抗偏头痛药物舒马曲坦（5-HT1A激动剂）对醋酸诱导的小鼠扭体反应的镇痛作用。舒马曲坦以剂量依赖性方式产生作用（1、5、10和20毫克/千克，皮下注射）。阿片拮抗剂纳洛酮（1毫克/千克，腹腔注射）未能逆转舒马曲坦诱导的镇痛作用。拟胆碱药毒扁豆碱（0.05毫克/千克，腹腔注射）增强了舒马曲坦的镇痛作用，而毒蕈碱拮抗剂阿托品（5毫克/千克，腹腔注射）则分别阻断了舒马曲坦的镇痛作用。将舒马曲坦的镇痛作用与另一种5-HT激动剂（5-HT1A）丁螺环酮进行了比较，丁螺环酮也产生了镇痛作用。与舒马曲坦镇痛作用一样，丁螺环酮的反应也以对阿托品敏感的方式被毒扁豆碱增强。此外，丁螺环酮增强了舒马曲坦的镇痛作用。这些观察结果表明，5-HT1A激动剂可能通过调节中枢胆碱能活性产生镇痛作用。
