Prokopenko R A, Mogilevich S E, Luik A I, Naydyenova I Y, Batrak G N, Hawryluk B R, Degtiar V Y
Biomedical Department, National Academy of Sciences of Ukraine.
Gen Physiol Biophys. 1995 Aug;14(4):349-57.
Effects of chlorpromazine, haloperidol (neuroleptics and calmodulin antagonists), and verapamil on rat platelet aggregation induced by thrombin, on calcium current in snail neurones and on both tonic tension of high potassium contracture and phasic contraction of isolated guinea-pig ureter preparations were studied. Moreover, droperidol, sulpiride and prazosine effects were studied for models of phasic contractility and platelet aggregation. Sulpiride and prazosine were ineffective, verapamil was ineffective on platelet aggregation, while droperidol was the most potent inhibitor of platelet aggregation. These results, the similarity revealed in the blockage of neuronal calcium current by neuroleptics and verapamil, and the potent inhibitory action of haloperidol and chlorpromazine on contractility and aggregation suggest that both phenothiazine and butyrophenone neuroleptics possess some properties of calcium antagonists and may also have intracellular sites of action other than calmodulin.
研究了氯丙嗪、氟哌啶醇(抗精神病药及钙调蛋白拮抗剂)和维拉帕米对凝血酶诱导的大鼠血小板聚集、蜗牛神经元钙电流以及高钾挛缩的强直张力和离体豚鼠输尿管标本的相性收缩的影响。此外,还研究了氟哌利多、舒必利和哌唑嗪对相性收缩性和血小板聚集模型的作用。舒必利和哌唑嗪无效,维拉帕米对血小板聚集无效,而氟哌利多是最有效的血小板聚集抑制剂。这些结果、抗精神病药和维拉帕米在阻断神经元钙电流方面显示出的相似性,以及氟哌啶醇和氯丙嗪对收缩性和聚集的强效抑制作用表明,吩噻嗪类和丁酰苯类抗精神病药都具有一些钙拮抗剂的特性,并且可能还具有除钙调蛋白以外的细胞内作用位点。