Effects on nociception of the Ca2+ and 5-HT antagonist dotarizine and other 5-HT receptor agonists and antagonists.

S Belcheva, V D Petkov, E Konstantinova, V V Petkov, E Boyanova
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Abstract

The effects of the Ca2+ and 5-HT1 and 5-HT2 receptor antagonist dotarizine and of some other agonists and antagonists of different 5-HT receptor subtypes administered alone or in combination with the 5-HT uptake inhibitor fluoxetine (FLU) on nociception were studied, using a foot-pressure method (analgesy-meter testing). Dotarizine (DOT) administered at a dose of 50 mg/kg for 3 days orally significantly increased the pain threshold. Fluoxetine (FLU) administered at a dose of 10 mg/kg for 3 days also significantly increased the pain threshold. The combination of DOT and FLU abolished the analgesic effects of the two drugs. The 5-HT1A and 5-HT1B/1C receptor agonists buspirone and m-CPP decreased the pain threshold. The antagonists of 5-HT1A(NAN-190),5-HT1/5-HT2(methysergide), 5-HT2 (ritanserin), and 5-HT3 (ondansetron) receptors as well as the agonists of 5-HT2(DOI) and 5-HT3 (mCPBG) receptors increased the pain threshold. Fluoxetine at a single dose of 10 mg/kg differently influenced the effects of the 5-HT agonists and antagonists on nociception. Comparison of the effects of dotarizine with the effects of some of the agonists and antagonists of 5-HT receptor subtypes on the nociceptive and other actions suggests the possibility of a therapeutic value of dotarizine as an antimigraine drug.

钙离子和5-羟色胺拮抗剂多巴胺和其他5-羟色胺受体激动剂和拮抗剂对伤害感觉的影响。
采用足压法(镇痛计试验)研究了Ca2+和5-HT1和5-HT2受体拮抗剂多他嗪以及其他一些不同5-HT受体亚型的激动剂和拮抗剂单独或与5-HT摄取抑制剂氟西汀(FLU)联合使用对伤害感觉的影响。Dotarizine (DOT)以50mg /kg的剂量口服3天,显著增加疼痛阈值。氟西汀(FLU)以10 mg/kg的剂量连续3天也显著增加疼痛阈值。DOT与FLU联合使用可消除两种药物的镇痛作用。5-HT1A和5-HT1B/1C受体激动剂丁螺环酮和m-CPP降低疼痛阈值。5-HT1A(NAN-190)、5-HT1/5-HT2(甲基塞吉胺)、5-HT2(利坦色林)和5-HT3(昂丹司琼)受体拮抗剂以及5-HT2(DOI)和5-HT3 (mCPBG)受体激动剂均可提高疼痛阈值。氟西汀单剂量10 mg/kg对5-HT激动剂和拮抗剂对伤害感觉的影响不同。将多塔利嗪与5-羟色胺受体亚型的一些激动剂和拮抗剂对痛觉和其他行为的影响进行比较,提示多塔利嗪作为抗偏头痛药物可能具有治疗价值。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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