Influence of a Selective 5HT1-Receptor Agonist GR43175 on Platelet Responsiveness
Influence of a Selective 5HT1-Receptor Agonist GR43175 on Platelet Responsiveness
复制标题
选择性 5HT1 受体激动剂 GR43175 对血小板反应性的影响
DOI：
10.1046/j.1468-2982.1995.1506472.x
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发表时间：
1995
期刊：
影响因子：
4.9
通讯作者：
A. Carolei
中科院分区：
文献类型：
--
作者：
M. Tozzi;C. Massimo;E. Tozzi;A. Mascioli;G. Matteis;A. Carolei
舒马曲坦，一种选择性5-HT 1受体激动剂，与血小板反应性的可能相互作用进行了研究。用舒马曲坦（1-100 μM）刺激富含血小板的血浆不会引起形状改变、聚集或血小板内胞浆钙水平的改变。用100 μM舒马曲坦预孵育血小板20分钟，可完全抑制20 μM 5-HT诱导的血小板聚集。在同一模型中，用4 μM腺苷5 '-二磷酸（ADP）（已知可诱导不可逆单相曲线的浓度）刺激血小板，可确定聚集反应的降低。1 μM ~ 50 μM舒马曲坦对5-HT和ADP诱导的聚集反应无影响。这些影响似乎不是由血小板钙稳态的改变决定的。舒马曲坦调节血小板反应性的可能性为评估血小板行为与偏头痛病理生理学之间的可能联系提供了进一步的方法。
The possible interaction of sumatriptan, a selective 5HT1-receptor agonist, with platelet responsiveness has been investigated. Stimulation of platelet rich plasma with sumatriptan (1–100 μM) did not induce shape change, aggregation or modification of intraplatelet cytosolic calcium levels. Total inhibition of aggregation induced by 20 μM 5HT was observed in platelets preincubated for 20 min with 100 μM sumatriptan. In the same model, platelet stimulation with 4 μM adenosine 5'-diphosphate (ADP), concentration known to induce an irreversible single-phase curve, determined a decrease of aggregatory response. Concentrations from I μM to 50 μM of sumatriptan did not influence the aggregatory response induced by 5HT and ADP. These effects appear not to be determined by modifications of platelet calcium homeostasis. The possibility to modulate platelet responsiveness by sumatriptan offers a further approach for evaluating the probable link between platelet behaviour and pathophysiology of migraine.