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临床经验提示,山莨菪碱(654-2)对心血管系统功能有比较明显的影响,但确切的作用机理尚未充分阐明。鉴于654-2的结构与经典的M-阻断剂阿托品相似,我们应用放射性配基结合试验检测了654-2对M-;α_1-、α_2-及β-受体结合的影响,并与阿托品,酚妥拉明,心得安等进行了比较。实验结果经计算机拟合,654-2阿托品及酚妥拉明抑制~3H-QNB与鼠心M-受体结合的IC_(50)分别为4.41×10~(-7),1.44×10~(-8)及2.60×10~(-8)抑制~3H-Prazosin与鼠心α_1-受体结合的IC_(50)分别为2.34×10~(-5),1.20×10~(-5)及5.70×10~(-8)M;抑制~3H-yohimbine
Clinical experience suggests that anisodamine (654-2) has a significant effect on cardiovascular system function, but the exact mechanism of action has not yet been fully elucidated. In view of the similar structure of 654-2 to the classic M-blocker atropine, we examined the effect of 654-2 on the binding of M-; a1-, a2-, and a-receptors by radioligand binding assays, , Phentolamine, propranolol, etc. were compared. The results of computer simulation, IC4 (50) of 654-2 atropine and phentolamine inhibition ~ 3H-QNB and mouse heart M-receptor binding were 4.41 × 10 -7, 1.44 × 10 ~ -8 and 2.60 × 10 -8 inhibited 3H-Prazosin binding to rat heart α 1 -receptor with IC50 values of 2.34 × 10 -5 and 1.20 × 10 -5 and 5.70 × 10 ~ (-8) M; inhibition ~ 3H-yohimbine