Fungal transformations of antihistamines: metabolism of methapyrilene, thenyldiamine and tripelennamine to N-oxide and N-demethylated derivatives.

Cerniglia, C E; Hansen, E B; Lambert, K J; Korfmacher, W A; Miller, D W

Cerniglia, C E; Hansen, E B; Lambert, K J; Korfmacher, W A; Miller, D W.

Afiliación

Cerniglia CE; National Center for Toxicological Research, Food and Drug Administration, Jefferson, Arkansas 72079.

Xenobiotica ; 18(3): 301-12, 1988 Mar.

Article en En | MEDLINE | ID: mdl-2898181

RESUMEN

1. Strains of the fungus Cunninghamella elegans ATCC 9245 and 36112 were tested for their ability to transform the antihistamines methapyrilene (I), thenyldiamine (II) and tripelennamine (III). 2. Antihistamine metabolites were isolated by h.p.l.c., and identified by their 1H-n.m.r. and mass spectral properties. 3. All three drugs were transformed by both C. elegans strains to N-oxidized and N-demethylated derivatives. Metabolism during 96 h of incubation amounted to 85% for (I), 64% for (II), and 83% for (III). Metabolites soluble in organic solvents amounted to 62% to 86% of the total metabolism; approximately 88% to 95% of the organic-soluble metabolites were N-oxide derivatives of each antihistamine.

Asunto(s)

Aminopiridinas/metabolismo; Antagonistas de los Receptores Histamínicos H1/metabolismo; Metapirileno/metabolismo; Mucorales/metabolismo; Piridinas/metabolismo; Tripelenamina/metabolismo; Biotransformación; Cromatografía Líquida de Alta Presión; Espectroscopía de Resonancia Magnética; Espectrometría de Masas; Metilación; Óxidos/metabolismo

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Tripelenamina / Aminopiridinas / Antagonistas de los Receptores Histamínicos H1 / Metapirileno / Mucorales Idioma: En Revista: Xenobiotica Año: 1988 Tipo del documento: Article Pais de publicación: Reino Unido

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