Novel carbamate metabolites of mofegiline, a primary amine monoamine oxidase B inhibitor, in dogs and humans
Identifieur interne : 004A77 ( Main/Curation ); précédent : 004A76; suivant : 004A78Novel carbamate metabolites of mofegiline, a primary amine monoamine oxidase B inhibitor, in dogs and humans
Auteurs : J. Dow [France] ; F. Piriou ; E. Wolf [France] ; B. D. Dulery [France] ; K. D. HaegeleSource :
- Drug metabolism and disposition [ 0090-9556 ] ; 1994.
Descripteurs français
- Pascal (Inist)
- Wicri :
- topic : Homme.
English descriptors
- KwdEn :
Abstract
Mofegiline or MDL 72,974A ((E)-4-fluoro-β-fluoromethylene benzene butanamine hydrochloride) is a selective enzyme-activated irreversible inhibitor of monoamine oxidase B, which is under development for use in the treatment of Parkinson's disease. Male beagle dogs were given single po (20 mg/kg) and iv (5 mg/kg) doses of [14C]-Mofegiline. Total radioactivity excreted in urine and feces over 96 hr was, respectively, 75.5±3.8 and 6.3±3.4% of the dose after po and 67.9±0.5 and 3.9±2.4% after iv administration. Unchanged drug in urine represented 3% of the dose after po and less than 1% after iv administration. Mofegiline was thus extensively metabolized in dogs, and urinary excretion was the major route of elimination of metabolites
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Pascal:94-0697054Le document en format XML
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<term>Human</term>
<term>Intraperitoneal administration</term>
<term>MAO inhibitor</term>
<term>Metabolism</term>
<term>Metabolite</term>
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<term>Chien</term>
<term>Animal</term>
<term>Homme</term>
<term>Antiparkinsonien</term>
<term>Voie orale</term>
<term>Voie intrapéritonéale</term>
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<front><div type="abstract" xml:lang="en">Mofegiline or MDL 72,974A ((E)-4-fluoro-β-fluoromethylene benzene butanamine hydrochloride) is a selective enzyme-activated irreversible inhibitor of monoamine oxidase B, which is under development for use in the treatment of Parkinson's disease. Male beagle dogs were given single po (20 mg/kg) and iv (5 mg/kg) doses of [<sup>14</sup>
C]-Mofegiline. Total radioactivity excreted in urine and feces over 96 hr was, respectively, 75.5±3.8 and 6.3±3.4% of the dose after po and 67.9±0.5 and 3.9±2.4% after iv administration. Unchanged drug in urine represented 3% of the dose after po and less than 1% after iv administration. Mofegiline was thus extensively metabolized in dogs, and urinary excretion was the major route of elimination of metabolites</div>
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