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  • Title: Biotransformation of N-methylcyclobarbital in vivo in rabbit and rat.
    Author: Miyano K, Shimodouzono Y, Toki S.
    Journal: Xenobiotica; 1985 May; 15(5):381-9. PubMed ID: 2863899.
    Abstract:
    Metabolism of N-methylcyclobarbital in the rabbit and rat has been studied in vivo for the purpose of comparison with the C5-methylated analogue, hexobarbital. In the rabbit, the main route of the metabolism of N-methylcyclobarbital is glucuronide formation after hydroxylation at the 3'-position of the parent compound. Dehydrogenation of the 3'-hydroxy product, a major pathway in the metabolism of hexobarbital, was a minor route in the case of N-methylcyclobarbital. In addition, a new type of metabolite, thought to be dihydroxylated products from spectral studies, was isolated. In the rat, there were almost no differences in the metabolic fates of N-methylcyclobarbital and hexobarbital. Profiles of metabolism of four analogous barbiturates (N-methylcyclobarbital, hexobarbital, cyclobarbital and norhexobarbital), which have a cyclohexene ring on the 5-carbon, reveal the contribution of alkyl substituents in the barbiturate ring on the bioavailability and metabolism of these compounds.
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