Cardiac action of KB-944, a new calcium antagonist

Arzneimittelforschung. 1982;32(9):1053-5.

Abstract

A comparative study was made between the cardiac action of diethyl 4-(benzothiazol-2-yl)benzylphosphonate (KB-944) and those of nifedipine, diltiazem and verapamil in anesthetized dogs and isolated right atria of guinea pigs. In anesthetized dogs, KB-944 caused a dose-dependent fall in mean blood pressure and dose-dependent increase in coronary sinus outflow. Coronary sinus outflow oxygen pressure was increased with increasing coronary sinus outflow; and consequently, the coronary arterio-venous oxygen difference was decreased. The cardiac output was slightly increased, while the myocardial oxygen consumption and myocardial work were reduced. In the isolated right atria of guinea pigs, KB-944 produced a decrease in spontaneous atria rate, and at the concentration of 10(-6) g/ml atrial standstill was seen in few preparations. The contractile force was decreased by KB-944. Especially, KB-944 exerted the weakest effect on contractile force among the tested drugs. These actions of KB-944 are very similar to those of nifedipine, diltiazem and verapamil.

MeSH terms

  • Anesthesia
  • Animals
  • Benzothiazoles
  • Calcium Channel Blockers / pharmacology*
  • Coronary Circulation / drug effects
  • Dogs
  • Guinea Pigs
  • Heart / drug effects*
  • Heart Rate / drug effects
  • Hemodynamics / drug effects
  • In Vitro Techniques
  • Myocardial Contraction / drug effects
  • Myocardium / metabolism
  • Oxygen Consumption / drug effects
  • Thiazoles / pharmacology*

Substances

  • Benzothiazoles
  • Calcium Channel Blockers
  • Thiazoles
  • fosfedil