A Comparative Study on the Effects of Disulfiram, Cyanamide and 1‐Aminocyclopropanol on the Acetaldehyde Metabolism in Rats

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Abstract
1‐aminocyclopropanol (ACP) is a potent inhibitor of aldehyde dehydrogenase (ALDH) in vivo and in vitro. Like cyanamide it has a rapid onset of action in vivo with the highest inhibition occurring after 2‐24 hrs. and a long duration of action like disulfiram with measurable inhibition after 144 hrs. All the three inhibitors decreased the activity of the mitochondrial low‐Km ALDH strongly in vivo, however, in markedly different doses. Cyanamide inhibited the high‐Km ALDH only in vivo, whereas in vitro, the high‐Km ALDH was unaffected by cyanamide but significantly inhibited by disulfiram and ACP. The inhibition produced by the inhibitors appeared to be irreversible. Acetaldehyde protected the low‐Km enzyme at different extents depending on the inhibitor used. The inhibition of ALDH in intoxicated and control rats and its relation to acetaldehyde oxidation and the disulfiram‐ethanol reaction are discussed.

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