Grima M, Decker N, Schwartz J
Arzneimittelforschung. 1986 Oct;36(10):1457-60.
The new positive inotropic agents sulmazole, piroximone, milrinone and 1,5-dihydro-6-chloro-3-methy-limidazo [2,1-b]quinazolone-2 enhance 22Na uptake in rat brain synaptosomes. In comparison, theophylline, a cyclic nucleotide phosphodiesterase inhibitor, has no effect on synaptosomal 22Na uptake. Tetrodotoxin inhibits the stimulation induced by the new inotropic agents. The quinazolone is about three times more potent than protoveratrine B and milrinone and ten times more potent than sulmazole and piroximone. There is a direct correlation between the 22Na uptake and the positive inotropic effect on guinea pig left atria of the new cardioactive drugs. The dose-response curves for synaptosomal 22Na uptake and for the inotropic effect on guinea pig left atria are parallel for sulmazole and the quinazolone drug, with first an increase and then a decrease in activity.
新型正性肌力药物舒马唑、匹罗昔酮、米力农和1,5-二氢-6-氯-3-甲基咪唑并[2,1-b]喹唑啉-2可增强大鼠脑突触体对22Na的摄取。相比之下，环核苷酸磷酸二酯酶抑制剂茶碱对突触体22Na摄取无影响。河豚毒素可抑制新型正性肌力药物所诱导的刺激作用。喹唑啉的效力约为原藜芦碱B和米力农的三倍，是舒马唑和匹罗昔酮的十倍。新型心脏活性药物对豚鼠左心房的正性肌力作用与22Na摄取之间存在直接相关性。舒马唑和喹唑啉类药物的突触体22Na摄取剂量-反应曲线与对豚鼠左心房的正性肌力作用剂量-反应曲线平行，活性先升高后降低。
