ANTAGONISM TOWARDS ENDOGENOUS ADENOSINE AND INHIBITION OF CGI-PDE IN THE CARDIAC EFFECTS OF AMRINONE, MILRINONE AND RELATED ANALOGS

被引：19

作者：

DORIGO, P

GAION, RM

BELLUCO, P

BOREA, PA

GUERRA, L

MOSTI, L

FLOREANI, M

CARPENEDO, F

机构：

[1] UNIV PADUA, DEPT PHARMACOL, LARGO E MENEGHETTI 2, I-35131 PADUA, ITALY

[2] UNIV GENOA, INST PHARMACEUT SCI, I-16132 GENOA, ITALY

[3] UNIV FERRARA, INST PHARMACOL, I-44100 FERRARA, ITALY

来源：

GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1992年 / 23卷 / 03期

关键词：

D O I：

10.1016/0306-3623(92)90124-3

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. The effect of amrinone, milrinone and of three milrinone analogues was tested on spontaneous chronotropic and inotropic activity of guinea-pig isolated atria, on the activity of cGMP-inhibited phosphodiesterase (cGI-PDE) from guinea-pig heart and on specific binding of n6-cyclohexyl[H-3]adenosine ([H-3]CHA) to R(i) adenosine receptors in guinea-pig atria. 2. The K(i)-values towards [H-3]CHA binding to R(i) receptors were linearly related to the EC50s for the increase in force of contraction but not to the EC50s for the increase in frequency of the atria. The K(i) values towards cGI-PDE were linearly related to the EC50s for the positive chronotropic effect.

引用

页码：535 / 541

页数：7

共 40 条

[1] CARDIOTONIC ACTIVITY OF MILRINONE, A NEW AND POTENT CARDIAC BIPYRIDINE, ON THE NORMAL AND FAILING HEART OF EXPERIMENTAL-ANIMALS [J].