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出 处:《药学学报》1990年第7期485-489,共5页Acta Pharmaceutica Sinica
摘 要:萘甲异喹(NI)呈浓度依赖性地降低离体豚鼠心房收缩力和频率。其拮抗豚鼠左房肌Iso正性肌力作用的PD2_2′值为5.4,Ver为5.8。NI10μmol/L明显降低豚鼠乳头肌收缩力;缩短快反应APD,以对APD_(20)影响最大,但不影响APA和V_(max)。对高K^+去极化慢反应动作电位,NI产生浓度依赖性负性肌力作用,同时明显降低APA,V_(max),缩短APD;提高细胞外液Ca^(2+)浓度可使其抑制作用逆转。结果提示NI具有钙通道阻滞作用。The effect of naphthylmethyl isoquinoline on amplitude of contraction and automaticity of guinea pig atria were investigated. The compound was found to markedly inhibit the force of contraction and automaticity in a concentration-dependent way. Propranolol competitively antagonized the effect of isoproterenol with-pA_2 of 7.5. Naphthylmethyl isoquinoline and verapamil antagonized isoproterenol, but in a noncompetitive manner with the pD_2' of 5.4 and 5.8, respectively. The effect of the compound on action potential and contractile force of guinea pig papillary muscles were also studied. It was shown to produce negative inotropic effects and shorten the fast action potential duration, but the maximal upstroke(Ⅴ_(max)) and amplitude of action potential were not affected. Thus, an excitation-contraction uncoupling was observed. It also depressed the amplitude. Ⅴ_(max) and duration of Ca^(2+)-mediated slow action potential induced by high K^+. Elevation of the CaCl_2 concentration from 2 to 5 mmol/L reversed its inhibition partially. These results indicate that naphthylmethyl isoquinoline has a blocking effect on calcium channels.
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