A comparison of in vivo and in vitro metabolites of the h1-antagonist n, n-dimethyl-n'-2-pyridyl-n'-(2-thienylmethyl)- 1,2-ethanediamine (methapyrilene) in the rat

S. S. Singer, W. Lijinsky, L. E. Kratz, N. Castagnoli Jr, J. E. Rose

Research output: Contribution to journalArticlepeer-review

Abstract

1. The H1-antagonist N, N-dimethyl-N'-2-pyridyl-N'-(2-thienylmethyl)- 1,2-ethanediamine (methapyrilene) is carcinogenic in rats. 2. The compound, which is inactive in short-term tests and does not bind to DNA, has been classified as a non-genotoxic carcinogen. 3. Studies have been made in vitro and in vivo in F344 and Sprague-Dawley rats. New metabolites include N-(N',N'-dimethylaminoethyl)-2-aminopyridine and the corresponding N'-oxide, a derivative in which methapyrilene is hydroxylated on the 5-position of the pyridine ring, 2-(N',N'-dimethylamino)-N-2'pyridylacetamide, N-(2-pyridyl)-N-2'thienylmethyl)aminoacetaldehyde, and 2-hydroxymethylthiophene. 4. Both strains of rat metabolize methapyrilene to reactive species which may be of importance in the carcinogenic process.

Original languageEnglish (US)
Pages (from-to)1279-1291
Number of pages13
JournalXenobiotica
Volume17
Issue number11
DOIs
StatePublished - 1987
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Toxicology
  • Pharmacology
  • Health, Toxicology and Mutagenesis

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