Zobrazeno 1 - 10
of 34
pro vyhledávání: '"K E, Thummel"'
Publikováno v:
Acta anaesthesiologica Scandinavica. 47(6)
Cytochrome P4502E1(CYP2E1)-mediated oxidation of halothane to a reactive intermediate (trifluoroacyl chloride) that covalently binds to hepatic proteins forming trifluoroacetylated neoantigens is believed to be the initiating event in a complex immun
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 29(11)
Under certain culture conditions, exposure of the human colon adenocarcinoma cell line Caco-2 to 1,25-(OH)(2)-D(3) induces expression of CYP3A4 to levels comparable to that in human small intestinal epithelium. To determine whether 1,25-(OH)(2)-D(3)
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 28(12)
Acetaminophen (APAP), a widely used analgesic and antipyretic agent, can cause acute hepatic necrosis in both humans and experimental animals when consumed in large doses. It is generally accepted that N-acetyl-p-benzoquinone imine (NAPQI) is the tox
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 28(9)
To determine the level of FMO1 protein present in human liver tissues, a monospecific antibody was prepared and a sensitive Western blotting procedure with enhanced chemiluminescence detection was developed. Human FMO1, purified from insect cells exp
Publikováno v:
Pharmaceutical research. 17(3)
The intestinal metabolism of some CYP3A substrates can be altered profoundly by co-administration of the potent inhibitor, ketoconazole. The present research was conducted to test the hypothesis that, unlike the inhibition kinetics observed with isol
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 291(1)
Disulfiram (DSF) is a mechanism-based inhibitor of cytochrome P-450 2E1 (CYP2E1), resulting in loss of CYP2E1 protein and activity, which may be useful in preventing CYP2E1-mediated xenobiotic toxicity. The duration of inhibition after a single DSF d
Publikováno v:
Pharmaceutical research. 16(8)
To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6 substrate, metoprolol, between microsomes prepared from human intestinal mucosa and from human live
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 27(6)
Disulfiram and its primary metabolite diethyldithiocarbamate are effective mechanism-based inhibitors of cytochrome P-450 2E1 (CYP2E1)1 in vitro. Single-dose disulfiram diminishes CYP2E1 activity in vivo and has been used to identify CYP2E1 participa
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 27(5)
The purpose of this work was to evaluate the effect of mutual unbound inhibitor and unbound enzyme depletion on the potency of three antifungal cytochrome P-450 (CYP)3A inhibitors with over 1000-fold range in enzyme affinity. Incubations were perform
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 289(2)
It has been suggested that the binding of a drug to plasma proteins will influence the intestinal extraction efficiency when drug is delivered to the mucosal epithelium via either the gut lumen or vasculature. We evaluated this hypothesis using cytoc