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| 題名: | Effects of Hemerocallis flava on motor activity and the concentration of central monoamines and its metabolites in rats |
| 作者: | Hsieh, MT;Ho, YF;Peng, WH;Wu, CR;Chen, CF |
| 貢獻者: | 藥學院藥化所;Hsieh, MT, CHINA MED COLL,INST CHINESE PHARMACEUT SCI,91 HSUEH SHIH RD,TAICHUNG,TAIWAN |
| 日期: | 1996 |
| 上傳時間: | 2010-09-24 15:06:12 (UTC+8) |
| 出版者: | ELSEVIER SCI IRELAND LTD |
| 摘要: | The effect of A02131-1 [3-(5'-hydroxymethyl-2'-furyl)-1-benzyl thieno (3,2-c)pyrazole], a cGMP-specific phosphodiesterase (PDE) inhibitor, on platelet function was investigated. The compound was found to inhibit the aggregation of and adenosine triphosphate (ATP) release from human platelet-rich plasma and washed platelets that were induced by aggregation inducing drugs such as arachidonic acid (AA), collagen, U46619, platelet-activating factor (PAF), adenosine diphosphate (ADP) and A23187, and the inhibitory effect was concentration-dependent. A02131-1 also disaggregated the preformed platelet aggregates induced by these inducers. Thromboxane B-2 (TXB(2)) formations caused by collagen, PAF, ADP, and A23187 were inhibited by A02131-1 at concentrations that did not affect the AA-induced formation of TXB(2) and prostaglandin D-2 (PGD(2)), A02131-1 suppressed both the generation of inositol 1,4,5-trisphosphate (IP3) and the increase of intracellular Ca2+ concentration stimulated by these aggregation inducers. A02131-1 was shown to increase the cAMP and cGMP levels in platelets and the extent was found to be dependent on concentration as well as time, A02131-1 increased the cAMP level much more slowly than the cGMP level. Activities of adenylate cyclase, guanylate cyclase, and PDEs (type I and III) were not altered by A02131-1. However, the activity of cGMP-specific PDE (type V) was inhibited by A02131-1, The antiplatelet aggregation activity and the effect on raising cAMP level of A02131-1 were both potentiated by prostaglandin E(1) (PGE(1)), In the mouse tail bleeding test, A02131-1 was clearly shown to be more effective than dipyridamole in prolonging the tail bleeding time of conscious mice. These data indicate that A02131-1 is a cGMP-specific PDE (type V) inhibitor in human platelets. (C) 1996 by The American Society of Hematology. |
| 關聯: | JOURNAL OF ETHNOPHARMACOLOGY 52(2):71-76 |
| 顯示於類別: | [藥物化學研究所] 期刊論文
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