Ca-agonists: a new class of inotropic drugs.

Basic Research in Cardiology
M BechemM Schramm

Abstract

The basic pharmacology of dihydropyridine Ca-agonists published so far (BAY k8644, CGP 28-392, H 160/51, YC 170, and 202-791) is described. The importance of the potency of the enantiomeres for the effect of a racemic compound is underlined. The Ca agonist prototype BAY k8644 leads to an increase of the maximal rate of rise of left ventricular pressure (LV(dP/dt)) and an increase of left ventricular stroke work in conscious dogs. When the vascular effects of BAY k8644 are counterbalanced by intravenous injection of sodium-nitroprusside, the left ventricular functions curves show markedly increased stroke work against the same mean arterial blood pressure at the same filling pressure. BAY k8644 stimulates the heart economically: the net efficiency in isolated working guinea-pig hearts is about 20%, identical to a stimulation by calcium or ouabain. Cardiotonic drugs acting via cAMP-dependent mechanisms like isoprenaline, amrinone, or pimobendane however, stimulate the heart about 1/3 less economically. The mechanism of action of Ca-agonists is explained from electrophysiological findings: Ca-agonistic dihydropyridines increase the open probability of the Ca-channels by a shift of the open-probability curve to more negative membra...Continue Reading

References

May 1, 1985·Pflügers Archiv : European journal of physiology·M Bechem, L Pott
Aug 15, 1985·European Journal of Pharmacology·G FranckowiakG Thomas
Nov 18, 1985·Life Sciences·M Schramm, R Towart
Aug 1, 1986·Naunyn-Schmiedeberg's Archives of Pharmacology·H NakayaM Kanno
May 1, 1987·Journal of Molecular and Cellular Cardiology·M Bechem, M Schramm
Jan 1, 1987·Annual Review of Pharmacology and Toxicology·D J Triggle, R A Janis
Jul 1, 1984·Journal of Molecular and Cellular Cardiology·M C Sanguinetti, R S Kass
Sep 1, 1984·Journal of Cardiovascular Pharmacology·K C PreussD C Warltier
Feb 14, 1984·Biochemical and Biophysical Research Communications·P ErneH Rogg
Jul 1, 1984·Physiological Reviews·H Rasmussen, P Q Barrett

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