Effect of DC-015, a novel potent and selective α1-adrenoceptor antagonist, comparison with prazosin on noradrenaline-induced platelet aggregation

M. H. Yen, Y. M. Lee, T. F. Huang, J. R. Sheu

研究成果: 雜誌貢獻文章

摘要

The antiplatelet activity of DC-015, a newly synthesized quinazoline derivative was determined in human platelet-rich plasma. From the binding studies, the Ki values of DC-015 for α1-, α2-adrenoceptors and 5-HT1, 5-HT2 receptors were about 0.21 (nM), 0.59 (μM), 0.59 (μM) and 0.38 (μM), respectively. On the other hand, the Ki values of prazosin for α1- and α2-adrenoceptors were about 0.19 (nM) and 4.8 (μM), respectively. Experimental results indicated that DC-015 dose-dependently inhibited noradrenaline (10 μM)-induced platelet aggregation in human platelet-rich plasma. At 20 μM, DC-015 would completely inhibit platelet aggregation induced by noradrenaline. A high concentration of prazosin (>30 mM) caused slight inhibition of aggregation. Furthermore, DC-015 (2 μM) significantly increased the cyclic AMP level in human platelet-rich plasma, whereas, prazosin significantly increased cyclic AMP level only at higher concentrations (100 μM). We can conclude that DC-015 inhibited noradrenaline-induced platelet aggregation mainly through binding to α2-receptor on platelets, resulting in inhibiting platelet aggregation.

原文英語
頁(從 - 到)93-98
頁數6
期刊Chinese Journal of Physiology
38
發行號2
出版狀態已發佈 - 1995
對外發佈Yes

ASJC Scopus subject areas

  • Physiology

指紋 深入研究「Effect of DC-015, a novel potent and selective α1-adrenoceptor antagonist, comparison with prazosin on noradrenaline-induced platelet aggregation」主題。共同形成了獨特的指紋。

  • 引用此