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Results for “Cardanolides”

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PubMed1975

Reversible inhibition of (Na+ + K+)-ATPase with a cardiac glycoside.

The effect of a semisynthetic cardiac glycoside, Actinogen (Ay22241), on Na+ + K+ - ATPase was studied. Ay22241 was found to be as an effective inhibitor of the enzyme as ouabain, Ay22241 inhibition was a time dependent process and was completely reversible. While ouabain inhibition was also time dependent, it was only partially reversible. This reversibility with Ay22241 should make it a useful tool in studying the mode of action of cardiac glycosides.

Adenosine Triphosphatases↗
PubMed1975

Effects of AY-22,241 (Actodigin) on electrical and mechanical activity of cardiac tissues.

AY-22,241 (Actodigin) is a new rapid-acting semisynthetic cardiotonic steroid. In experiments on contractility of cat papillary muscle, Actodigin (2 times 10(-7) to 4 times 10(-6) M) produced a dose-dependent positive inotropic effect, a marked increase in the maximum rate of force development, and no change in resting tension. Electrophysiologic studies performed with microelectrode techniques on isolated Purkinje fibers superfused with Tyrode solution, revealed dose-dependent decreases in resting membrane potential, action potential amplitude and duration, and the maximum rate of rise of phase 0 (Vmax). Purkinje fibers superfused with extracorporeally circulated blood from a donor dog receiving 0.075 mg/kg/min Actodigin showed small decreases in resting membrane potential preceding the onset of donor premature ventricular contractions. Progressive decreases in resting membrane potential, action potential amplitude and duration, and Vmax accompanied donor ventricular tachycardia. All effects were rapidly reversible, and compared to ouabain, equi-inotropic concentrations of Actodigin caused significantly less electrophysiologic toxicity.

Animals↗