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Metabolism of paraldehyde to acetaldehyde by rat liver microsomes
Abstract:
Paraldehyde (PAL) was shown to be metabolized to acetaldehyde (AcH) by rat liver microsomes in vitro only when the cofactors for the cytochrome P-450 system were present. Microsomes from phenobarbital treated rats significantly increased the amount of AcH produced from PAL. Attempts to inhibit this reaction by addition of SKF-525A to the incubation medium resulted in augmentation of the AcH generated, very likely due to the metabolic deethylation of SKF-525A itself to AcH. Rats pretreated with D-penicillamine and then given PAL excreted 2,5,5-trimethylthiazolidine-4-carboxylic acid (TTCA)-a condensation product of AcH and D-penicillamine-in the urine. These results strongly suggest that PAL is metabolized in vivo by the hepatic microsomal system giving rise to AcH as a metabolite.
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