A comparison ofin vivoandin vitrometabolites of the H1-antagonistN, N-dimethyl-N'-2-pyridyl-N'-(2-thienylmethyl)- 1,2-ethanediamine (methapyrilene) in the rat
| Autor: | J. E. Rose, W. Lijinsky, S. S. Singer, N. Castagnoli, L. E. Kratz |
|---|---|
| Rok vydání: | 1987 |
| Předmět: |
Male
Chromatography Gas Stereochemistry Health Toxicology and Mutagenesis Metabolite Methapyrilene Aminopyridines In Vitro Techniques Biology Toxicology Biochemistry chemistry.chemical_compound In vivo Pyridine medicine Animals Biotransformation Chromatography High Pressure Liquid Carcinogen Glucuronidase Pharmacology Rats Inbred Strains General Medicine Rats Inbred F344 In vitro Rats chemistry Microsomes Liver Derivative (chemistry) DNA medicine.drug |
| Zdroj: | Xenobiotica. 17:1279-1291 |
| ISSN: | 1366-5928 0049-8254 |
| Popis: | 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 included 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|