论文部分内容阅读
维拉帕米的一个不对称碳原子带有各不相同的4个侧链,构成右旋异构体(D-体)和左旋异构体(L-体).市售维拉帕米为两者的外消旋混合物(RM).异构体药效学的差异Bayer等将离体猫心乳头肌置于含各种浓度D-体和L-体维拉帕米的生理溶液中,发现L-体的负性肌力作用比D-体强;而且发现刺激频率加快时L-体的负性肌力作用增强,D-体的负性肌力作用在刺激频率减慢时最强.即两种异构体作用强度不等,而且作用机制各异.有人认为D-体可抑制钠通道.
One of the asymmetric carbon atoms in verapamil has four different side chains, forming the dextrorotary (D-body) and the L-isomer (L-body) Racemic mixture of both (RM). Differences in Isomer Pharmacodynamics Bayer et al. Placed the isolated cat papillary muscles in physiological solutions containing various concentrations of D- and L-verapamil, It was found that the negative inotropic effect of L-body was stronger than that of D-body, and the negative inotropic effect of L-body was enhanced when the stimulation frequency was accelerated. The negative inotropic effect of D-body was the strongest when the stimulation frequency slowed down . That is, the intensity of the two isomers varies, and the mechanism of action varies. Some people think that D-body can inhibit sodium channels.