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New Inhibitors of Alcohol Dehydrogenase: Studies in Vivo and in Vitro in the Rat
Author(s) -
Delmas Catherine,
Blanquat Georges de Saint,
Freudenreich Charles,
Bielimann JeanFranCois
Publication year - 1983
Publication title -
alcoholism: clinical and experimental research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.267
H-Index - 153
eISSN - 1530-0277
pISSN - 0145-6008
DOI - 10.1111/j.1530-0277.1983.tb05456.x
Subject(s) - in vivo , ethanol , chemistry , alcohol dehydrogenase , aldehyde dehydrogenase , alcohol , in vitro , biochemistry , enzyme , pharmacology , acetaldehyde , intraperitoneal injection , biology , microbiology and biotechnology
Two compounds bearing an amide group, pbutoxyphenyl acetamide (BPA) and N‐(p‐butoxybenzyl)formamide (BBF) were studied as inhibitors of alcohol dehydrogenase (ADH) and their action compared with that of 4‐methyl‐pyrazole (4‐MP), a known Inhibitor of this enzyme. In vitro studies on pure horse liver ADH showed that BPA and BBF were noncompetitive inhibitors with respect to ethanol and that their K, vaiues were 22 and 0.14 pm, respectively. The apparent K, values of BPA and BBF for rat liver ADH were found to be 90 and 2.3. pm, respectively (noncompetitive inhibition). Several in vivo experiments were carried out in the rat. Administration intraperitoneaily of the substances (480 μmol/kg) 1 hr before intra‐peritoneal injection of alcohol (2 g/kg body weight) led to a significant decrease in ethanol catabollsm. Injection of the substances at 460 pmol/kg brought about a decrease in rat liver ADH activity, but the activity of mitochondrial aldehyde dehydrogenase was only decreased in animals treated with BBF.