N-Methylation of nicotine enantiomers by human liver cytosol

Autor:	Peter A. Crooks, C S Godin
Rok vydání:	1988
Předmět:	Male Nicotine Metabolite Guinea Pigs Pharmaceutical Science In Vitro Techniques Methylation chemistry.chemical_compound Cytosol medicine Animals Humans Ammonium Pharmacology Chemistry Substrate (chemistry) Stereoisomerism Rats Turnover number Liver Biochemistry Stereoselectivity medicine.drug
Zdroj:	Journal of Pharmacy and Pharmacology. 40:153-154
ISSN:	2042-7158 0022-3573
Popis:	Incubation of human liver cytosol with either R-(+)-[3H-N′CH3]nicotine or S-(−)-[3H-N′CH3]nicotine results in the formation of the corresponding N-methyl quaternary ammonium metabolite. A substrate stereoselectivity was observed in that the turnover number for the methylation of the S-(−)-isomer was 0.25 pmol mg 1 protein h−1, whereas that for the R-(+)-isomer was 2.11. The latter substrate exhibited an apparent Km value of 20.1 μM. Nicotine N-methylation appears to be species-dependent, since rat liver homogenates contained no ‘nicotine N-methyl-transferase’ activity, whereas with guinea-pig liver homogenates, a substrate specificity for only R-(+)-nicotine was observed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e292b28069ddae4fb65178a05d234972 https://doi.org/10.1111/j.2042-7158.1988.tb05207.x Zobrazit plný text záznamu Plný text