R. Deitrich, P. Troxell, W. Worth
Dec 15, 1976
Citations
3
Influential Citations
122
Citations
Quality indicators
Journal
Biochemical pharmacology
Abstract
Abstract Cyanamide (H 2 N—C N) is effective as an agent to treat alcoholism presumably because it inhibits aldehyde dehydrogenase. In this study it was found that, in vivo , cyanamide is a very potent inhibitor of liver aldehyde dehydrogenases. but less effective against the brain enzymes. The ED 50 for liver was found to be 8 mg/kg when given intraperitoneally. The inhibition diminishes with time but is measurable for at least 24 hr, even though the bulk of the 14 C-labeled cyanamide is excreted within 6 hr. Cyanamide is not effective when added to the assay mixture in vitro , suggesting that a metabolite is the inhibitor in vivo . A urinary metabolite has been isolated and partially characterized. It is an acid with a p K a' of 3.9 and an extinction coefficient of 1.72 × 10 3 in base at 219 nm; the compound apparently retains the cyano group. However, it does not inhibit the enzyme in vitro .