1-(4-methoxyphenyl)piperazine has been researched along with Arrhythmias--Cardiac* in 1 studies
1 other study(ies) available for 1-(4-methoxyphenyl)piperazine and Arrhythmias--Cardiac
Article | Year |
---|---|
Synthesis, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents.
A series of novel arylpiperazines have been prepared in an attempt to incorporate both class II (beta-receptor blocking) and class III antiarrhythmic properties in a single molecule. The key step in the preparation of the new compounds involves a regioselective heterocyclic ring formation. All but four compounds significantly prolonged action potential duration in canine cardiac Purkinje fibers (class III activity). All but one of the compounds demonstrated beta-receptor affinity in a competitive binding assay and three had beta 1-receptor selectivity. Compared to sotalol, a reference class II/III agent, arylpiperazine 7a (4-[(methylsulfonyl)amino]-N-[(4- phenylpiperazin-2-yl)methyl]benzamide) demonstrated beta 1-selectivity and was 1 order of magnitude more potent in the in vitro class III and the beta 1-receptor screens. Compound 7a was evaluated further and found to be effective in preventing programmed electrical stimulation-induced arrhythmias in conscious dogs (class III activity) and against epinephrine-induced arrhythmias in halothane anesthetized dogs (class II activity). Topics: Action Potentials; Adrenergic beta-Antagonists; Animals; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; Benzamides; Binding, Competitive; Dogs; Electric Stimulation; Electrophysiology; Epinephrine; Heart; Molecular Structure; Piperazines; Purkinje Fibers; Receptors, Adrenergic, beta; Sotalol; Structure-Activity Relationship | 1992 |