[Pharmacological research on bonnecor and its metabolites].
The antiarrhythmic and local anesthetic effects of 4 metabolites (G 491, ABD 19-200, ABD 19-199, ABD 19-205) of a new antiarrhythmic drug bonnecor (GS-015) were studied on the models of arrhythmias induced by aconitine (rats), barium chloride (rabbits), electrical fibrillation (cats), ouabain (dogs) as well as surface anesthesia (rabbit cornea). The side effects on the cardiovascular system were investigated on anesthetized cats. As compared with the original compound (bonnecor) metabolites G 491 and ABD 19-200 on different test models exhibited the action which on the antiarrhythmic terms was 2-14 times less weak than that of bonnecor but the metabolites were less toxic. Metabolites ABD 19-199 and ABD 19-205 reach the degree of effectiveness of bonnecor but their toxicity is higher. It follows from the above that the beneficial effect of bonnecor is not achieved by its metabolites.
Poppe
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VEB Pharmazeutisches Kombinat GERMED, Dresden, DDR.
Heer
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Barch
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R
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000188:drug therapy; D003984:Dibenzazepines / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D011817:Rabbits; D051381:Rats; D014693:Ventricular Fibrillation / Q000188:drug therapy / Q000209:etiology
D000889:Anti-Arrhythmia Agents; D003984:Dibenzazepines; C048166:tiracizine
Farmakologicheskoe issledovanie bonnekora i ego metabolitov.