Bartel' V, Gluza E, Markvardt F
Farmakol Toksikol. 1976 May-Jun;39(3):296-301.
With a view of decoding the mechanisms of their action the effect of papaverine, chlorpromazine and imipramine produced on a number of blood platelets hemostatic functions was studied. All the three drugs suppress in a characteristic fashion the aggregation on blood platelets caused by thrombin in the Tyrode solution and in a plasma defibrilated by heating, as well as by collogen and ADP in the citrated plasma. Unlike chlorpromazine and imipramine papaverine exerts a strong inhibiting action on the phosphodiesterase activity. Chlorpromazine and imipramine suppress the absorption of serotonin and retraction more intensively than this is done by papaverine and call forth morphological changes in the blood platelets that proceed parallel with changes in the intensity of the photodiffusion and liberation of endogenous serotonin. It is postulated that chlorpromazine and imipramine manifest their inhibitory effect through nonspecific damage of the blood platelets membranes, whereas papaverine does this through exchange of adenine-nucleotides and, especially, of 3',5'-AMP.
为了解其作用机制,研究了罂粟碱、氯丙嗪和丙咪嗪对多种血小板止血功能的影响。这三种药物均以独特方式抑制由凝血酶在台氏液中、加热去纤维蛋白的血浆中以及在枸橼酸盐血浆中的胶原和ADP所引起的血小板聚集。与氯丙嗪和丙咪嗪不同,罂粟碱对磷酸二酯酶活性有强烈抑制作用。氯丙嗪和丙咪嗪比罂粟碱更强烈地抑制5-羟色胺的摄取和血小板回缩,并引起血小板形态变化,这些变化与光扩散强度和内源性5-羟色胺释放的变化平行发生。据推测,氯丙嗪和丙咪嗪通过对血小板膜的非特异性损伤来表现其抑制作用,而罂粟碱则通过腺嘌呤核苷酸尤其是3',5'-AMP的交换来实现。