[普罗托品对兔血小板功能的影响]

[Effect of protopine on rabbit platelet function].

作者信息

Ma G Y, Zhang Z Z, Chen Z H

机构信息

Department of Pharmacology, Kunming Medical College, China.

出版信息

Zhongguo Yao Li Xue Bao. 1994 Jul;15(4):367-71.

PMID:7801784

Abstract

Protopine (Pro) inhibited dose-dependently rabbit platelet aggregation induced by ADP, arachidonic acid (AA), collagen, or aggregoserpentin of Trimeresurus mucrosquamatus venom (TMVA) in vitro. Their IC50 were 25.3, 30.5, 46.9, 33.4 mumol.L-1, respectively. Pro 10, 20 mg.kg-1 iv also inhibited the platelet aggregation induced by these inducers. The effects (maximal at 5 min) lasted 1 h. By using fluorophotometry and RIA, it was seen that Pro suppressed the release of 5-HT from platelets during aggregation induced by collagen, AA, or TMVM in vitro. Pro did not block the formation of thromboxane A2 during aggregation induced by AA and did not increase the content of cAMP in rabbit platelet, but increased the content of cGMP in rabbit platelets. The antiplatelet effect of Pro may be related to an increase cGMP in rabbit platelets and the suppression of the release of the active substances from platelets.

摘要

原阿片碱（Pro）在体外能剂量依赖性地抑制由ADP、花生四烯酸（AA）、胶原蛋白或竹叶青蛇毒（TMVA）的凝集素诱导的兔血小板聚集。它们的半数抑制浓度（IC50）分别为25.3、30.5、46.9、33.4 μmol·L-1。静脉注射10、20 mg·kg-1的Pro也能抑制这些诱导剂所诱导的血小板聚集。其作用（在5分钟时达到最大）持续1小时。通过荧光光度法和放射免疫分析发现，Pro在体外能抑制胶原蛋白、AA或TMVM诱导的血小板聚集过程中5-羟色胺（5-HT）的释放。Pro在AA诱导的聚集过程中不阻断血栓素A2的形成，也不增加兔血小板中环磷酸腺苷（cAMP）的含量，但能增加兔血小板中环磷酸鸟苷（cGMP）的含量。Pro的抗血小板作用可能与兔血小板中cGMP的增加以及血小板活性物质释放的抑制有关。