NQ-Y15 Inhibits the Calcium Mobilization by Elevation of Cyclic AMP in Rat Platelets

概要

論文の詳細を見る
2-[(4-Cyanophenyl)amino]-3-chloro-1, 4-naphthalenedione(NQ-Y15)is a dual action drug which acts as a thromboxane A_2(TXA_2)synthase inhibitor and TXA_2/PGH_2 receptor antagonist. In the present study, we examined the effects of NQ-Y15 on Ca^2+ mobilization, which is the common event in various types of platelet activation, in arachidonic acid(AA)-stimulated rat platelets. The elevation of cytosolic Ca^2+ concentration([Ca^2+]_i)induced by AA was inhibited by NQ-Y15 in a concentration-dependent manner. This inhibition-effect of NQ-Y15 was found to be based on the suppression of the rise in [Ca^2+]_i by the inhibition of both Ca^2+ release from internal stores and Ca^2+ influx from the extracellular space. Our successive trial was focused on the role of cyclic AMP(cAMP) in the action of NQ-Y15, because cAMP was reported to be increased by dual action drugs such as picotamide and to inhibit the increase in [Ca^2+]_i. NQ-Y15 was confirmed to increase cAMP in AA-stimulated rat platelets. These results suggested that NQ-Y15 might inhibit the rise in [Ca^2+]_i in AA-treated rat platelets by increasing cAMP, which is involved in the inhibition of platelet activation.
公益社団法人日本薬学会の論文
2001-05-01