Toremifene metabolism in rat, mouse and human liver microsomes: identification of alpha-hydroxytoremifene by LC-MS.
Biomed Chromatogr
; 16(5): 361-3, 2002 Aug.
Article
en En
| MEDLINE
| ID: mdl-12210510
ABSTRACT
The in vitro metabolism of toremifene has been studied in liver microsomal preparations from rat, mouse and human sources using high-performance liquid chromatography-electrospray ionisation mass spectrometry (HPLC-ESIMS). The metabolites detected were N-desmethyltoremifene (m/z 392), 4-hydroxytoremifene (m/z 422), 4'-hydroxytoremifene (m/z 422) and toremifene N-oxide m/z 422). In addition, a new polar metabolite with a protonated molecule at m/z 422 has been detected in all three species. The compound was identified by tandem MS-MS as alpha-hydroxytoremifene, an analogue of alpha-hydroxytamoxifen. The results showed that alpha-hydroxylation is a common feature of tamoxifen and toremifene metabolism and that alpha-hydroxytamoxifen is unlikely to be the reactive metabolite responsible for the hepatocarcinogenesis in rat, as widely believed.
Buscar en Google
Colección:
01-internacional
Asunto principal:
Microsomas Hepáticos
/
Cromatografía Líquida de Alta Presión
/
Toremifeno
/
Moduladores Selectivos de los Receptores de Estrógeno
/
Espectrometría de Masa por Ionización de Electrospray
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Biomed Chromatogr
Año:
2002
Tipo del documento:
Article
País de afiliación:
Reino Unido