| Autor: |
Leinweber FJ, Loh AC, Szuna AJ, Carbone JJ, Williams TH, Sasso GJ, Tilley JW, Pace D, Dahlen P, Kovacs JL, et. al. |
| Jazyk: |
angličtina |
| Zdroj: |
Xenobiotica; the fate of foreign compounds in biological systems [Xenobiotica] 1983 May; Vol. 13 (5), pp. 287-94. |
| DOI: |
10.3109/00498258309052266 |
| Abstrakt: |
A microsomal metabolite of cibenzoline, 4,5-dihydro-2-(2,2-diphenylcyclopropyl)-1H-imidazole butanedioate, was identified by n.m.r. as the 4,5-dehydro analogue, 2-(2,2-diphenylcyclopropyl)-1H-imidazole. Three dogs dosed orally with 13.8 mg/kg 14C-cibenzoline base excreted 1.8-3.5% of the dose as this metabolite in the urine. Mean plasma concentrations of cibenzoline reached a peak of 1.5 micrograms/ml at 2 h while mean concentrations of the metabolite of 0.4-0.5 micrograms/ml were found between 2 and 7 h. The metabolite was synthesized and found to decrease the frequency of ventricular premature depolarizations in conscious dogs having a two-stage occlusion of the left anterior descending coronary artery performed 48 h before. It did not inhibit ventricular arrhythmia in rats induced by i.v. infusion of aconitine. Thus, in contrast to cibenzoline, the metabolite does not appear to be a true antiarrhythmic agent. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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