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Titolo:
ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF A NEW, C-14-LABELED OXAZOLIDINONE MAO-A INHIBITOR IN RAT AND DOG
Autore:
NAITOH T; MISHIMA M; KAWAGUCHI S; MATSUI K; ANDOH T; KAGEI K; KAKIKI M; YUZURIHA T; HORIE T;
Indirizzi:
EISAI & CO LTD,DEPT REGULATORY COMPLIANCE,BUNKYO KU,KOISHIKAWA 4-6-10TOKYO 11288 JAPAN EISAI & CO LTD,TSUKUBA RES LABS TSUKUBA IBARAKI 30026 JAPAN
Titolo Testata:
Xenobiotica
fascicolo: 10, volume: 27, anno: 1997,
pagine: 1053 - 1070
SICI:
0049-8254(1997)27:10<1053:ADMAEO>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
MONOAMINE-OXIDASE INHIBITORS; ADVERSE REACTIONS; E2011;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
10
Recensione:
Indirizzi per estratti:
Citazione:
T. Naitoh et al., "ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF A NEW, C-14-LABELED OXAZOLIDINONE MAO-A INHIBITOR IN RAT AND DOG", Xenobiotica, 27(10), 1997, pp. 1053-1070

Abstract

1. After oral administration of C-14-labelled )benzothiazol-6-yl]-5-metoxymethyl-2-oxazolidinone (E2011) at a dose of 1 mg/kg, the blood level of radioactivity leached a maximum concentration (C-max) of 0.545 mu g eq./ml after 0.25 h in the rat and of 0.900 mu g eq./ml after 0.5h in the dog. In dog plasma, C-max for radioactivity and unchanged E2011 were 0.862 mu g eq./ml and 0.650 mu g/ml respectively with corresponding T-max (time at C-max) of 0.75 and 0.25 h. The unchanged drug indog plasma was below the detection limit (5 ng/ml plasma) after 24 h.2. The tissue levels of radioactivity were measured at 0.25 (T-max), 6, 24, and 168 h after administration to the rat and at 0.5 (T-max), 24, and 168 h in the dog. The radioactivity was distributed in all tissues examined at T-max in the rat and dog. The radioactivity levels of the cerebral cortex in the rat and dog were 26 and 36% of the plasma level at T-max. The radioactivity in tissues decreased at almost the same rate as that in plasma. Plasma protein binding of the unchanged drug in the rat in vitro were about 70% in the range of 0.1-10 mu g/ml, and those in the dog were about 45 % in the same concentration range. 3. Cumulative excretion of radioactivity in the rat was 74.5 % in urineand 22.5 % in faeces after 7 days. In the dog, 55.5 and 36.5 % of theradioactivity administered were excreted in urine and faeces respectively after 7 days. The biliary excretion of radioactivity in the cannulated rat was 23.0% within 48 h. 4. In tie analysis of plasma and tissues of the rat and dog, the radioactivity for the unchanged drug was much higher than metabolites. In tie analysis of urine, the same metabolites were detected in the rat and dog, and the radioactivity of a metabolite, IM1, was the highest in the both animals. Eight metabolites were detected in the plasma, tissues and excreta of the rat, and four metabolites in the dog. 5. In conclusion, the absorption, distribution,metabolism and excretion of C-14-labelled E2011 in the rat and dog have been established, and only minor differences were observed between these species.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 06:15:19