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  1. Ketoconazole and the modulation of multidrug resistance-mediated transport in Caco-2 and MDCKII-MDR1 drug transport models.

    Xenobiotica 38(2):107 (2008) PMID 18197554

    The hypothesis tested was that ketoconazole can modulate P-glycoprotein, thereby altering cellular uptake and apparent permeability (P(app)) of multidrug-resistant substrates, such as cyclosporin A (CSA) and digoxin, across Caco-2, MDCKII-MDR1, and MDCKII wild-type cell transport models. (3)H-CS...
  2. Quantitative analysis of aryl hydrocarbon receptor activation using fluorescence-based cell imaging--a high-throughput mechanism-based assay for drug discovery.

    Xenobiotica 38(1):1 (2008) PMID 18098060

    Early identification of toxicity associated with new chemical entities is important for reducing compound attrition in late stage drug discovery. Activation of the aryl hydrocarbon receptor (AhR) by xenobiotics is a recognised mechanism of toxicity: the AhR mediates most, if not all, of the seri...
  3. Effect of the anticoagulant ethylenediamine tetra-acetic acid (EDTA) on the estimation of pharmacokinetic parameters: A case study with tigecycline and ciprofloxacin.

    Xenobiotica 38(1):76 (2008) PMID 17963190

    Tigecycline and ciprofloxacin were employed as the model compounds to study the effect of the anticoagulant ethylenediamine tetra-acetic acid (EDTA), which is used during plasma sample preparations, on the determination of pharmacokinetic parameters. The pharmacokinetic parameters were determine...
  4. Nicotine metabolism and urinary elimination in mouse: in vitro and in vivo.

    Xenobiotica 38(1):34 (2008) PMID 18098062

    This study aimed at elucidating the in vivo metabolism of nicotine both with and without inhibitors of nicotine metabolism. Second, the role of mouse CYP2A5 in nicotine oxidation in vitro was studied as such information is needed to assess whether the mouse is a suitable model for studying chemi...
  5. Heredity mode of genetic polymorphism in aldehyde oxidase activity in Donryu strain rats.

    Xenobiotica 38(1):98 (2008) PMID 18098066

    Donryu strain rats show genetic polymorphisms in the aldehyde oxidase gene, resulting in the phenotypic expression of ultrarapid metabolizers with homozygous nucleotide sequences (337G, 2604C), extensive metabolizers with heterozygous nucleotide sequences (377G/A, 2604C/T), and poor metabolizers...
  6. Disposition and metabolism of dipropyl disulphide in vivo in rat.

    Xenobiotica 38(1):87 (2008) PMID 18098065

    The metabolism of dipropyl disulphide (DPDS), a sulphur compound from onion, was investigated in vivo in the rat. A single dose (200 mg kg(-1)) was administered by gastric intubation and the time courses of DPDS and its metabolites were followed over 48 h by gas chromatography coupled with mass ...
  7. In vivo effects of Urtica urens (dwarf nettle) on the expression of CYP1A in control and 3-methylcholanthrene-exposed rats.

    Xenobiotica 38(1):48 (2008) PMID 18098063

    The in vivo effects of the intraperitoneal administration of an Urtica urens L. (dwarf nettle) seed extract were examined on the hepatic, pulmonary, and renal cytochrome P450-dependent monooxygenase activities of rats co-administered with 3-methylcholanthrene (MC). Urtica extract was administere...
  8. Identification of cytochrome P450 enzymes responsible for N -dealkylation of a new oral erectogenic, mirodenafil.

    Xenobiotica 38(1):21 (2008) PMID 18098061

    The purpose of this paper is to characterize the cytochrome P450 (CYP) enzymes involved in the metabolism of a new oral erectogenic, mirodenafil, to a major circulating active metabolite, N-dehydroxyethyl-mirodenafil, and to investigate the inhibitory potential of mirodenafil on seven CYP enzyme...
  9. Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination.

    Xenobiotica 38(1):62 (2008) PMID 18098064 PMCID PMC3691104

    The authors recently reported the increased oral clearance of labetalol in pregnant women. To elucidate the mechanism of the elevated oral clearance, it was hypothesized that female hormones, at the high concentrations attainable during pregnancy, enhance hepatic metabolism of labetalol. Labetal...
  10. CYP3A4 and CYP3A5 catalyse the conversion of the N-methyl-D-aspartate (NMDA) antagonist CJ-036878 to two novel dimers.

    Xenobiotica 37(12):1408 (2007) PMID 17943661

    CJ-036878, N-(3-phenethoxybenzyl)-4-hydroxybenzamide, was developed as an antagonist of the N-methyl-D-aspartate receptor NR2B subunit. Two dimeric metabolites, CJ-047710 and CJ-047713, were identified from the incubation mixture with CJ-036878 in human liver microsomes (HLM). The identification...