Cardiac Na+ channel activation as a positive inotropic principle.

Journal of Cardiovascular Pharmacology
G Scholtysik

Abstract

This article reviews the relation of cardiac cellular Na+ load and increased force of contraction. Digitalis glycosides and naturally occurring Na+ channel activators are considered. DPI201-106 was described as the first synthetic organic molecule with cardioselective Na+ channel-activating properties and investigated in clinical studies. Its pharmacology is reviewed. DPI 201-106 prolongs the open state of cardiac Na+ channels. This effect represents the primary mechanism of its positive inotropic effect. The involvement of cAMP is excluded. Ca2+ antagonistic and local anaesthetic effects are assumed to contribute advantageously to the pharmacodynamic profile of DPI 201-106. Chemically and pharmacologically related to DPI 201-106 is the new compound SDZ 210-921 for which original results are presented. It is concluded that DPI 201-106 represents the lead structure of a new class of cardiotonics with selective cardiac Na+ channel activation. DPI 201-106 and related compounds may serve as promising tools in the investigation of cardiac Na+ channel-gating dynamics, in addition to their therapeutic potential.

Citations

Feb 15, 1994·European Journal of Pharmacology·D S KrafteA M Ezrin
May 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·D S KrafteA M Ezrin
Jan 1, 1992·Circulation Research·J J MatsudaE F Shibata
Nov 26, 2004·American Journal of Physiology. Heart and Circulatory Physiology·Weiqun ShenMitchell I Steinberg
May 21, 1998·Journal of Cardiovascular Pharmacology·J Müller-EhmsenR H Schwinger
Aug 22, 2003·Cardiovascular Drug Reviews·Kanigula MubagwaBodo Brandts
Dec 31, 2021·Archiv der Pharmazie·Grigory V Mokrov

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