Schraven E, Trottnow D, Fiedler V B
Arzneimittelforschung. 1976 Feb;26(2):200-4.
The coronary-active drug 3-2-diethylaminoethyl)-4-methyl-7-(carbethoxy-methoxy)-2-oxo-1,2-chromene-hydrochloride (carbocromen, Intensain) is known to be an inhibitor of phosphodiesterase (PDE). After intravenous as well as after intraduodenal application of therapeutic doses carbocromen increases in vivo the cAMP-contents of the hearts of rats (by up to 30%) and dogs (up to 50%). This effect is dose related. Correlations between the pharmacokinetic properties and metabolic actions of carbocromen and its influence on the adenylcyclase system are discussed.
已知冠状动脉活性药物3-(2-二乙氨基乙基)-4-甲基-7-(乙氧羰基甲氧基)-2-氧代-1,2-色烯盐酸盐(卡波铬,心脉舒通)是一种磷酸二酯酶(PDE)抑制剂。静脉注射以及十二指肠内给予治疗剂量的卡波铬后,可使大鼠心脏(增加高达30%)和犬心脏(增加高达50%)的体内环磷酸腺苷(cAMP)含量升高。这种效应与剂量相关。本文讨论了卡波铬的药代动力学特性和代谢作用之间的关系及其对腺苷酸环化酶系统的影响。