[The anti-arrhythmic effect of the selective sigma-receptor antagonist DuP 734 [1-(cyclopropylmethyl)-4-(2'-(4''-fluorophenyl)-2'-oxoethyl)piper idine HBr]].
It was demonstrated on models of epinephrine-, CaCl2-, and aconitine-induced arrhythmias that the sigma-receptor antagonist DuP734 possesses high antiarrhythmic activity in a dose of 1 mg/kg. The sigma-receptor agonist-(+)SKF10,047 promoted the development of ventricular fibrillation. Atropine had no effect on the antiarrhythmic properties of DuP734. "Chemical sympathectomy" of the myocardium with the ganglion-blocking agent hexamethonium also did not affect the proarrhythmic properties of (+)SKF10,047. It is supposed that selective sigma-receptor blocking agents may be highly effective antiarrhythmic drugs.
Maslov
L N
LN
Krylatov
A V
AV
Lishmanov
Iu B
IuB
D000157:Aconitine; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000627:therapeutic use*; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000188:drug therapy; D002122:Calcium Chloride; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D004837:Epinephrine; D008024:Ligands; D008297:Male; D010620:Phenazocine / Q000031:analogs & derivatives / Q000627:therapeutic use; D010880:Piperidines / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar; D017480:Receptors, sigma / Q000819:agonists / Q000037:antagonists & inhibitors / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000627:therapeutic use*
D000889:Anti-Arrhythmia Agents; D008024:Ligands; D010880:Piperidines; D017480:Receptors, sigma; D012702:Serotonin Antagonists; C012134:SK&F 10047; C078773:DuP 734; D010620:Phenazocine; D002122:Calcium Chloride; D000157:Aconitine; D004837:Epinephrine