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  1. MRP class of human ATP binding cassette (ABC) transporters: historical background and new research directions.

    Xenobiotica 38(7-8):833 (2008) PMID 18668432

    1. The adenosine triphosphate (ATP) binding cassette (ABC) transporters form one of the largest protein families encoded in the human genome, and more than 48 genes encoding human ABC transporters have been identified and sequenced. It has been reported that mutations of ABC protein genes are cau...
  2. Bile acid transporters in health and disease.

    Xenobiotica 38(7-8):1043 (2008) PMID 18668439

    In recent years the discovery of a number of major transporter proteins expressed in the liver and intestine specifically involved in bile acid transport has led to improved understanding of bile acid homeostasis and the enterohepatic circulation. Sodium (Na(+))-dependent bile acid uptake from po...
  3. Comparative evaluation of absorption, distribution, and excretion of YM758, a novel If channel inhibitor, between albino and non-albino rats.

    Xenobiotica 38(5):527 (2008) PMID 18421625

    1. YM758 is a novel If channel inhibitor for the treatment of stable angina and atrial fibrillation. The absorption, distribution, and excretion of YM758 have been investigated in albino and non-albino rats after a single oral administration of (14)C-YM758 monophosphate. 2. YM758 was well absorb...
  4. Induction of cytochrome P450s by terpene trilactones and flavonoids of the Ginkgo biloba extract EGb 761 in rats.

    Xenobiotica 38(5):465 (2008) PMID 18421621

    1. Ginkgo biloba is one of the most popular herbal medicines worldwide due to its memory-enhancing and cognition-improving effects. The current study was designed to investigate the effects of five major constituents (bilobalide, ginkgolide A, B, quercetin, and kaempferol) in the standardized G....
  5. Pharmacokinetics and metabolism of KW-4490, a selective phosphodiesterase 4 inhibitor: difference in excretion of KW-4490 and acylglucuronide metabolites between rats and cynomolgus monkeys.

    Xenobiotica 38(5):511 (2008) PMID 18421624

    1. The pharmacokinetics and metabolism of KW-4490, a selective phosphodiesterase 4 inhibitor, were investigated in rats and monkeys. After oral administration, KW-4490 was rapidly absorbed, and then its plasma concentrations apparently declined with half-lives of approximately 5 h in rats and 3....
  6. In vitro drug-drug interaction studies with febuxostat, a novel non-purine selective inhibitor of xanthine oxidase: plasma protein binding, identification of metabolic enzymes and cytochrome P450 inhibition.

    Xenobiotica 38(5):496 (2008) PMID 18421623

    1. The potential for drug-drug interactions with febuxostat was examined in the following three in vitro systems: the characteristics of the binding of febuxostat to human plasma proteins; identification of the cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes participating in ...
  7. Identification of human cytochrome P450 enzymes involved in the metabolism of IN-1130, a novel activin receptor-like kinase-5 (ALK5) inhibitor.

    Xenobiotica 38(5):451 (2008) PMID 18421620

    1. The in vitro metabolism of 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide (IN-1,130), a selective activin receptor-like kinase-5 (ALK5) inhibitor and a candidate drug for fibrotic disease, was studied. 2. The cytochrome P450s (CYPs) responsible for metaboli...
  8. Prediction of metabolic clearance of diclofenac in adjuvant-induced arthritis rats using a substrate depletion assay.

    Xenobiotica 38(5):482 (2008) PMID 18421622

    1. The purpose of this study was to evaluate drug clearance measured by the metabolic intrinsic clearance (CL(int)) in a substrate depletion assay in comparison with the in vivo clearance (CL(tot)) observed in adjuvant-induced arthritis (AA) rats. 2. After intravenous administration of diclofena...
  9. Metabolism of prazosin in rat and characterization of metabolites in plasma, urine, faeces, brain and bile using liquid chromatography/mass spectrometry (LC/MS).

    Xenobiotica 38(5):540 (2008) PMID 18421626

    1. Prazosin, 2-[4-(2-furanoyl)-piperazin-1-yl]-4-amino-6,7-dimethoxyquinazoline, is an antihypertensive agent that has been used safely since 1976 and is currently being investigated for the treatment of post-traumatic stress disorder. The in vivo metabolism of prazosin in rat was first reported...
  10. Disposition and metabolism of the colchicine derivative [14C]-ZD6126 in rat and dog.

    Xenobiotica 38(4):399 (2008) PMID 18340564

    1. The tissue distribution, disposition and metabolism of ZD6126, a novel vascular targeting agent, were investigated in rat and dog. This paper comprises the findings of several investigations, including rat quantitative whole-body autoradiography (QWBA), rat and dog balance and metabolism (bot...
  11. Pharmacokinetic characterization of hydroxylpropyl-beta-cyclodextrin-included complex of cryptotanshinone, an investigational cardiovascular drug purified from Danshen (Salvia miltiorrhiza).

    Xenobiotica 38(4):382 (2008) PMID 18340563

    1. The study aimed to investigate the pharmacokinetics of cryptotanshinone in a hydroxylpropyl-beta-cyclodextrin-included complex in dogs and rats. 2. Animals were administrated the inclusion complex of cryptotanshinone and the concentrations of cryptotanshinone and its major metabolite tanshino...
  12. Effect of gender, dose, and time on 3-(3,5-dichlorophenyl)-2,4-thiazolidinedione (DCPT)-induced hepatotoxicity in Fischer 344 rats.

    Xenobiotica 38(4):435 (2008) PMID 18340566 PMCID PMC2922973

    1. The thiazolidinedione ring present in drugs available for type II diabetes can contribute to hepatic injury. Another thiazolidinedione ring-containing compound, 3-(3,5-dichlorophenyl)-2,4-thiazoli-dinedione (DCPT), produces liver damage in rats. Accordingly, the effects of gender, dose, and t...
  13. In vivo approach for the evaluation of mechanism-based inhibition of cytochrome P450 3A in rats.

    Xenobiotica 38(4):368 (2008) PMID 18340562

    1. There have been no reports showing that the area under the concentration-time curve (AUC) of a probe drug is elevated due to mechanism-based inhibition (MBI) of drug-metabolizing enzymes in animals. This study ascertained that mechanism-based inhibitors reported to induce drug-drug interactio...
  14. Dietary salt does not influence the disposition of verapamil enantiomers in relation to efflux transporter ABCB1 genetic polymorphism in healthy Korean subjects.

    Xenobiotica 38(4):422 (2008) PMID 18340565

    To evaluate the effects of dietary salt on the stereoselective disposition of verapamil enantiomers in relation to the transporter ABCB1 2677GG/3435CC and 2677TT/3435TT haplotypes, ten healthy subjects were asked to take diets of three different salt levels for 7 days in a randomized, three-way ...
  15. Prediction of metabolic clearance using fresh human hepatocytes: comparison with cryopreserved hepatocytes and hepatic microsomes for five benzodiazepines.

    Xenobiotica 38(4):353 (2008) PMID 18340561

    1. Predictions of in vivo intrinsic clearance from cryopreserved human hepatocytes may be systematically low. In the current study, the metabolite kinetics of a series of CYP3A4 substrates (benzodiazepines) in fresh human hepatocytes from five donors, via a major UK supplier, were investigated a...
  16. Pharmacokinetics and tissue distribution of 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide; a novel ALK5 inhibitor and a potential anti-fibrosis drug.

    Xenobiotica 38(3):325 (2008) PMID 18274960

    The authors investigated the pharmacokinetics and metabolism of 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide (IN-1130), a novel ALK5 inhibitor, which suppresses renal and hepatic fibrosis, and also exerts anti-metastatic effects on breast cancer-bearing MMTV...
  17. Preclinical absorption, distribution, metabolism and excretion (ADME) characterization of ICAM1988, an LFA-1/ICAM antagonist, and its prodrug.

    Xenobiotica 38(3):340 (2008) PMID 18274961

    Intercellular adhesion molecule (ICAM)-1988 is a small molecule lymphocyte function-associated antigen-1 (LFA-1) antagonist being considered for its anti-inflammatory properties. Following intravenous administration of ICAM1988, clearances in mice, rats, dogs, and monkeys were 17.8, 3.31, 15.4, ...
  18. Non-invasive method to detect induction of CYP3A4 in chimeric mice with a humanized liver.

    Xenobiotica 38(3):239 (2008) PMID 18274954

    Chimeric mice with a humanized liver have been previously established by the transplantation of human hepatocytes to urokinase-type plasminogen activator/severe combined immunodeficiency mice. A non-invasive method to detect the induction of cytochrome P450 (CYP) 3A4 was evaluated in chimeric mi...
  19. In vitro metabolism of KBH-A40, a novel delta-lactam-based histone deacetylase (HDAC) inhibitor, in human liver microsomes and serum.

    Xenobiotica 38(3):281 (2008) PMID 18274957

    1. The metabolism of KBH-A40, a novel delta-lactam-based histone deacetylase (HDAC) inhibitor, was investigated in vitro using human liver microsomes and serum. After 60-min incubation in human liver microsomes with beta-nicotinamide adenine dinucleotide phosphate (NADPH) or uridine diphosphate ...
  20. Metabolism and related human risk factors for hepatic damage by usnic acid containing nutritional supplements.

    Xenobiotica 38(3):264 (2008) PMID 18274956

    Usnic acid is a component of nutritional supplements promoted for weight loss that have been associated with liver-related adverse events including mild hepatic toxicity, chemical hepatitis, and liver failure requiring transplant. To determine if metabolism factors might have had a role in defin...