Detection and mass spectrometric characterization of the major urinary and fecal metabolites of 9-methyl-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]-quinolizine in the rat
Articolo
Data di Pubblicazione:
1995
Citazione:
Detection and mass spectrometric characterization of the major urinary and fecal metabolites of 9-methyl-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]-quinolizine in the rat / A. Sparatore, R. Maffei Facino, C. Canu Boido, V. Boido, F. Sparatore, E. Arlandini. - In: EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS. - ISSN 0378-7966. - 20:2(1995), pp. 135-144.
Abstract:
The metabolic fate of 9-methyl 1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizine (MIQ), a compound with promising pharmacological action on the CNS system, was investigated in the rat after an oral dose of 200 mg/kg, the maximal tolerated dose. Urine and feces were collected, exhaustively extracted with organic solvents and the metabolites detected by TLC analysis. The structures of the isolated metabolites were characterized by several mass spectrometry techniques (FD, EI, CI) and, in some cases, confirmed by synthesis. The major metabolic pathways of MIQ in the rat involve: C-oxidation of the methyl group in position 9 to a primary alcohol and to a carboxylic acid, N-oxidation of basic nitrogen and C-oxidation of the quinolizidine nucleus, probably at position 7.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Animals; Mass Spectrometry; Hydrogen-Ion Concentration; Spectrophotometry, Ultraviolet; Quinolizines; Magnetic Resonance Spectroscopy; Oxidation-Reduction; Rats; Rats, Sprague-Dawley; Biotransformation; Chromatography, Thin Layer; Feces; Central Nervous System Agents; Male
Elenco autori:
A. Sparatore, R. Maffei Facino, C. Canu Boido, V. Boido, F. Sparatore, E. Arlandini
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