Huang J, Dai Y, Qiu Y T, Hong X, Huang J Z, Yu F, Dai D Z
Research Division of Pharmacology, China Pharmaceutical University, Nanjing, China.
Zhongguo Yao Li Xue Bao. 1996 Jan;17(1):66-8.
To compare the kinetics of positive inotropism between ibopamine (Ibo) and ouabain (Oua).
The isolated right papillary muscle of cat was used to assess the positive inotropic effects by cummulative concentrations of Ibo and Oua. The maximal effects was recognized as the contraction just before the appearance of spontaneous contraction. A Hill equation was developed by using lg [E/(Emax-E)] vs lg C.
The S value of Ibo was smaller than that of Oua, causing C95/C5 (ratio of concentrations producing 95%/5% of Emax) of Ibo (264) elevenfold as large as Oua (22.9). Comparing with Oua, concentrations of Ibo initiating effects were lower, the slope was smaller, and higher concentrations were required for producing maximal effect. During drug concentration declining, the effect-concentration curve of Ibo showed a counter-hysteresis loop, more remarkable than Oua.
The changes in positive inotropism of Ibo against drug concentrations were less than those of Oua.
比较异波帕明(Ibo)和哇巴因(Oua)正性肌力作用的动力学。
采用猫离体右乳头肌,通过累积增加Ibo和Oua的浓度来评估正性肌力作用。最大效应被认为是在自发收缩出现之前的收缩。使用lg [E/(Emax - E)]对lg C建立希尔方程。
Ibo的S值小于Oua,导致Ibo的C95/C5(产生Emax的95%/5%的浓度比)(264)是Oua(22.9)的11倍。与Oua相比,Ibo产生作用的起始浓度较低,斜率较小,产生最大效应需要更高的浓度。在药物浓度下降期间,Ibo的效应-浓度曲线显示出反滞后环,比Oua更明显。
Ibo正性肌力作用随药物浓度的变化小于Oua。