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

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)93-98
Number of pages6
JournalChinese Journal of Physiology
Volume38
Issue number2
Publication statusPublished - 1995
Externally publishedYes

Keywords

  • α-adrenoceptor
  • DC-015
  • platelet aggregation

ASJC Scopus subject areas

  • Physiology

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