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Analgesic effect of morphine glucuronides.
The analgesic effect of morphine-6-glucuronide was 3 to 4 times as potent and approximately 2 times as long in duration as that of morphine when injected subcutaneously when injected intracerebrally in mice, but morphine-3-glUCuronide had no effect.
Species difference of site-selective glucuronidation of morphine.
Species difference in glucuronidation of morphine was studied using mice, rats, guinea pigs and rabbits in vivo and in vitro and a remarkable species difference was observed in the urinary excretion of the M-6-G.
Participation of cytochrome P450-2B and -2D isozymes in the demethylenation of methylenedioxymethamphetamine enantiomers by rats.
The results indicate that cytochrome P450 isozymes belonging to the CYP2D subfamily catalyze demethylenation with low Km values and that the reaction occurring with high Kmvalues is likely to be mediated by members of the CyP2B family, but with the possible participation of other phenobarbital-inducible isoforms.
Species differences in metabolism of codeine: urinary excretion of codeine glucuronide, morphine-3-glucuronide and morphine-6-glucuronide in mice, rats, guinea pigs and rabbits.
The results indicate that codeine is metabolized in all four species by glucuronidation and by oxidative N- and O-demethylation, but the quantitative excretions of metabolites were quite different in different species.
Formation of highly analgesic morphine-6-glucuronide following physiologic concentration of morphine in human brain.
The results suggest that endogenous morphine is converted to its 6-glucuronide, a more highly analgesic substance than the parent compound, to suppress effectively pain symptoms in humans.
Estrogen-dependent regulation of the expression of hepatic Cyp2b and 3a isoforms: assessment using aromatase-deficient mice.
Cyp3a11 is suppressed by estrogen, the expression of female-specific Cyp3a41 is programmed by neonatal and/or infantile exposure to estrogen, and endogenous estrogen plays little, if any, role in the mechanism by which PB induces Cyp2b10.
Cytochrome P450 1A1 (CYP1A1) inhibitor alpha-naphthoflavone interferes with UDP-glucuronosyltransferase (UGT) activity in intact but not in permeabilized hepatic microsomes from
Results suggest that a UGT isoform(s) involved in 3-OH-B(a)P glucuronidation is interfered by a CYP1A inhibitor via a mechanism dependent on the intact nature of microsomal membranes in MC-treated rats.