Metapramine (Timaxel) was oxidised by hepatic microsomes from rat and by biomimetic chemical systems; vanadyl acetylacetonate-iodylbenzene, phthalocyanin-iron II-iodosylbenzene, meso tetraphenyl porphyrine-iron III chloride-iodosylbenzene and Fenton's reagent. The major metabolite in all cases was the monodemethylated product formed by oxydative removal of the methyl group on the endocyclic nitrogen atom.
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The antidepressant metapramine is a low-affinity antagonist at N-methyl-D-aspartic acid receptors.
Neuropharmacology
June 1997
Rhône Poulenc Rorer, Centre de Recherche de Vitry-Alfortville, Vitry-sur-Seine, France.
Metapramine, a pharmacological compound with antidepressant activity in humans, was tested for possible antiglutamatergic activity, in vitro. We investigated the effects of metapramine on the N-methyl-D-aspartic acid (NMDA) receptor complex, by determining whether this compound would interfere with the binding of [3H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine ([3H]TCP) to rat cortical membranes in the presence of either glycine NMDA, or both. Metapramine in the micromolar range inhibited the binding of [3H]TCP in the presence of both NMDA and glycine (IC50 = 1.
View Article and Find Full Text PDFAntinociceptive activity of metapramine in mice. Relationship with its pharmacokinetic properties.
Life Sci
February 1992
Laboratoire de Pharmacologie et Pharmacie Clinique, Faculté de Pharmacie, CHRU, Clermont-Ferrand, France.
The antinociceptive effect of acutely and chronically (every brain elimination half-life time) administered metapramine, a tricyclic antidepressant without anticholinergic or cardiotoxic effects, was studied in three different pain tests. In the hot plate test, its action was more potent when jumping was used as a pain parameter (acute ED50 = 19 +/- 3 mg/kg, i.p.
View Article and Find Full Text PDFMetapramine (Timaxel) and his three major metabolites (19148 RP, 23669 RP, 19749 RP) have been determined in the plasma of 18 depressed inpatients treated by the antidepressant drug (12 women and 6 men; 7 are smokers and 11 non-smokers). In a steady state, interindividual variability is very important, especially for 23669 RP. No significant correlation exists between normalized doses (mg.
View Article and Find Full Text PDFMetabolism of metapramine in vitro by chemical model systems and rat liver microsomes.
Arzneimittelforschung
December 1989
Laboratoire de Chimie Organique, Faculté de Pharmacie de Lyon, France.
Metapramine (Timaxel) was oxidised by hepatic microsomes from rat and by biomimetic chemical systems; vanadyl acetylacetonate-iodylbenzene, phthalocyanin-iron II-iodosylbenzene, meso tetraphenyl porphyrine-iron III chloride-iodosylbenzene and Fenton's reagent. The major metabolite in all cases was the monodemethylated product formed by oxydative removal of the methyl group on the endocyclic nitrogen atom.
View Article and Find Full Text PDFHigh performance liquid chromatographic determination of fluvoxamine in human plasma.
Biomed Chromatogr
July 1989
Laboratoire de Toxicologie, Faculte de Pharmacie, Lille, France.
A method has been developed for the separation and measurement of fluvoxamine in human plasma by high performance liquid chromatography. The method uses metapramine as an internal standard and provides a limit of detection of about 1.5 ng/mL for fluvoxamine.
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