A novel methylthio metabolite of s-triazolo[3,4-a]phthalazine, a lead compound for the development of antianxiety drugs, in rats.
Life Sci
; 74(1): 29-36, 2003 Nov 21.
Article
en En
| MEDLINE
| ID: mdl-14575810
ABSTRACT
When s-triazolo[3,4-a]phthalazine (Tri-P) was orally administered in rats, a more lipophilic metabolite M-1 than the parent compound was isolated from the urine. The metabolite M-1 was identified as 7-methylthio Tri-P by means of high resolution MS and two-dimensional NMR spectrometry. Furthermore, the 7-methylthio conjugate was generated from the parent compound Tri-P in isolated rat hepatocytes. Although the contribution of the intestinal microflora to the formation of methylthio metabolite has been pointed out so far, the limited data in this study lead us to conclude that the liver plays a role in all metabolic reactions of Tri-P to its 7-methylthio conjugate in rats.
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Banco de datos:
MEDLINE
Asunto principal:
Ftalazinas
/
Ansiolíticos
/
Triazoles
/
Hepatocitos
Límite:
Animals
Idioma:
En
Revista:
Life Sci
Año:
2003
Tipo del documento:
Article
País de afiliación:
Japón