Ghelardini C, Galeotti N, Nicolodi M, Donaldson S, Sicuteri F, Bartolini A
Department of Preclinical and Clinical Pharmacology, University of Florence, Italy.
Int J Clin Pharmacol Res. 1997;17(2-3):105-9.
The antinociceptive effect of the antimigraine drug sumatriptan was assessed in mice (hot-plate and abdominal constriction tests). Antinociception induced by sumatriptan (10-30 mg kg-1 i.p.) was prevented by the muscarinic antagonist atropine (5 mg kg-1 i.p.), the ACh-depletor hemicolinium-3 (1 microgram per mouse i.c.v.) and the 5-HT1A antagonist NAN-190 (0.5 mg kg-1 i.p.). Naloxone, CGP-35348 and reserpine administered in doses suitable for blocking analgesia respectively induced by morphine, baclofen and clomipramine did not modify sumatriptan antinociception. On the basis of the above findings, we can deduce that sumatriptan was able to induce antinociception by increasing cholinergic neurotransmission through the stimulation of 5-HT1A receptors.
在小鼠中（热板和腹部收缩试验）评估了抗偏头痛药物舒马曲坦的镇痛作用。毒蕈碱拮抗剂阿托品（5 mg kg-1腹腔注射）、乙酰胆碱耗竭剂半胱氨酸-3（每只小鼠1微克脑室内注射）和5-HT1A拮抗剂NAN-190（0.5 mg kg-1腹腔注射）可阻断舒马曲坦（10-30 mg kg-1腹腔注射）诱导的镇痛作用。分别给予适合阻断吗啡、巴氯芬和氯米帕明诱导的镇痛作用剂量的纳洛酮、CGP-35348和利血平，并未改变舒马曲坦的镇痛作用。基于上述发现，我们可以推断舒马曲坦能够通过刺激5-HT1A受体增加胆碱能神经传递来诱导镇痛作用。
