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4-Nitrocatechol production from rho-nitrophenol by rat liver

J Chrastil and JT Wilson

Time course studies of rho-nitroanisole O-demethylation revealed formaldehyde production in excess of rho-nitrophenol (PNP) and 4- nitrocatechol (NTC) formation by rat liver microsomes. This indicated that these products (PNP, NTC) were metabolised further. The hydroxylation reaction PNP yields NTC showed substrate and product inhibition and a requirement for reduced nicotinamide adenine dinucleotide phosphate and O2 and was localized in liver microsomes. It was strongly activated by ascorbic acid, cysteine, adenosine triphosphate or hydroxylamine in vitro and enhanced by phenobarbital treatment in vivo. Mercapturic derivatives were metabolized to the corresponding hydroxy compounds with the same speed as their parent compounds. Both PNP and NTC were metabolized to the corresponding glucuronide and sulfate conjugates. On the other hand, the PNP or NTC glucuronides and sulfates were metabolized with liver microsomes to PNP and NTC.

Volume 193, Issue 2, pp. 631-638, 05/01/1975
Copyright © 1975 by American Society for Pharmacology and Experimental Therapeutics







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 Molecular Interventions Drug Metabolism and Disposition

Copyright © 1975 by the American Society for Pharmacology and Experimental Therapeutics.