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

作者信息

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

机构信息

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

出版信息

Xenobiotica. 1988 Mar;18(3):301-12. doi: 10.3109/00498258809041666.

DOI:10.3109/00498258809041666
PMID:2898181
Abstract
  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.
摘要

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