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新型抗偏头痛药物5-羟色胺受体拮抗剂曲普坦对血小板聚集的作用

[Effect of the new antimigraine drug serotonin receptor antagonist tropoxin on platelet aggregation].

作者信息

Vasil'eva T M, Petrukhina G N, Miftakhova N T, Makarov V A, Gan'shina T S, Bezhanian S G, Mirzoian R S

出版信息

Eksp Klin Farmakol. 2005 May-Jun;68(3):30-3.

PMID:16047677
Abstract

The effect of the new antimigraine drug tropoxin - the serotonin receptor (5-HT2) antagonist - on the human platelet aggregation in vitro induced by ADP (1 x 10(-5) M) and epinephrine (2.5 x 10(-6) M) was studied. Tropoxin reliably inhibited the ADP-induced platelet aggregation in a concentration range of 0.01 - 7 mg/ml. A significant inhibition effect with respect to the epinephrine-induced platelet aggregation was observed in a drug concentration range of 2 - 7 mg/ml, although a reliable antiaggregant activity was also observed below 2 mg/ml. A bolus administration of tropoxin (10 mg/kg) in rabbits decreased the ADP-induced platelet aggregation ex vivo by a factor of 1.2 - 1.4. The effect appeared 45 min after treatment and was observed during subsequent 30 min.

摘要

研究了新型抗偏头痛药物托罗辛(一种5-羟色胺受体(5-HT2)拮抗剂)对ADP(1×10⁻⁵M)和肾上腺素(2.5×10⁻⁶M)体外诱导的人血小板聚集的影响。托罗辛在0.01 - 7mg/ml的浓度范围内能可靠地抑制ADP诱导的血小板聚集。在2 - 7mg/ml的药物浓度范围内观察到对肾上腺素诱导的血小板聚集有显著抑制作用,尽管在2mg/ml以下也观察到了可靠的抗聚集活性。兔静脉注射托罗辛(10mg/kg)可使离体ADP诱导的血小板聚集降低1.2 - 1.4倍。该效应在治疗后45分钟出现,并在随后的30分钟内持续观察到。

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Eksp Klin Farmakol. 2005 May-Jun;68(3):30-3.
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