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离体兔胸主动脉条标本,测定8205对CaCl_2、JE引起收缩的量—效曲线及对单剂量KCl所致收缩的影响。结果表明,8205能使CaCl_2和NE的量—效曲线右移,并使最大反应压低,呈非竞争性拮抗,IC_(50)分别为13μmol/L和51μmol/L。8205也能抑制高K~+(67.1mmol/L)引起肌条的收缩反应,其IC_(50)为35.4μmol/L。与已知钙拮抗剂Ver比较,8205对三种激动剂收缩肌条的抑制作用与Ver湘似,但较弱。
Thoracic aortic strips were isolated from rabbit and measured the effect of 8205 on the contractile response induced by CaCl 2 and JE and the effect on contractility caused by single dose of KCl. The results showed that 8205 could shift the dose-response curves of CaCl 2 and NE to the right and depress the maximal response, showing non-competitive antagonism. The IC 50 values were 13μmol / L and 51μmol / L, respectively. 8205 also inhibited the contractile response of muscle strips induced by high K ~ + (67.1mmol / L) with IC50 of 35.4μmol / L. Compared with the known calcium antagonist Ver, 8205 has similar inhibitory effects on verotrophic contractions, but weaker.