Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.

abstract：:In vivo percutaneous absorption of emedastine difumarate was investigated in rats and compared with rat skin in vitro. Since emedastine entering the systemic circulation is mostly excreted in bile, we first came up with the method of collecting bile with a minimal skin incision. In vivo skin permeation of the drug was...

journal_title：Drug metabolism and pharmacokinetics

authors： Harada S,Yamashita F,Hashida M

更新日期：2005-10-01 00:00:00

abstract：:The present study was undertaken to characterize the transport of (3-methyl-His(2)) thyrotropin-releasing hormone ([(3)H]MeTRH) across the blood-brain barrier in mice and the effects of thyrotropin-releasing hormone (TRH) and its analogues (taltirelin and montirelin) on the transport and brain distribution. Integratio...

journal_title：Drug metabolism and pharmacokinetics

authors： Urayama A,Yamada S,Ohmori Y,Deguchi Y,Uchida S,Kimura R

更新日期：2003-01-01 00:00:00

abstract：:Nrf2 plays a central role in the response to xenobiotics and oxidative stress. The activation of Nrf2 induces the expression of drug-metabolizing enzymes (DMEs) and is important for cytoprotection. Keap1 is a widely accepted proteasome-dependent regulator of Nrf2. Keap1 was reported to be absent in Caenorhabditis eleg...

journal_title：Drug metabolism and pharmacokinetics

authors： Siswanto FM,Oguro A,Arase S,Imaoka S

更新日期：2020-10-01 00:00:00

abstract：:Bioavailability and therapeutic outcome of treatment with HIV-protease inhibitors depends on intestinal and hepatic transporter-enzyme interplay. Liver transport of HIV protease inhibitors (saquinavir, darunavir) was assessed in the presence of aged garlic extract, because the HIV-infected often consume garlic supplem...

journal_title：Drug metabolism and pharmacokinetics

authors： Berginc K,Trontelj J,Kristl A

更新日期：2010-01-01 00:00:00

abstract：:We performed a caffeine (N-3-methyl-13C) breath test (CafeBT) to determine whether it can be employed to identify caffeine metabolism-associated single nucleotide polymorphisms. The study included 130 healthy adults (mean age: 21.9 years). Saliva was collected using an Oragene®•DNA saliva collection kit. Breath sample...

journal_title：Drug metabolism and pharmacokinetics

authors： Ishii M,Ishii Y,Nakayama T,Takahashi Y,Asai S

更新日期：2020-06-01 00:00:00

abstract：:A novel method for the prediction of drug-drug interaction has been established based on the in vitro metabolic stability in the "serum incubation method" using cryopreserved human hepatocytes suspended in 100% human serum. As a novel approach, the inhibitory effect of inhibitors on the metabolism of substrates during...

journal_title：Drug metabolism and pharmacokinetics

authors： Shibata Y,Takahashi H,Chiba M,Ishii Y

更新日期：2008-01-01 00:00:00

abstract：:Methotrexate (MTX), a drug used for the treatment of certain cancers as well as rheumatoid arthritis, sometimes induces serious interstitial lung injury. Although lung toxicity of MTX is related to its accumulation, the information concerning MTX transport in the lungs is lacking. In this study, we investigated the me...

journal_title：Drug metabolism and pharmacokinetics

authors： Kawami M,Miyamoto M,Yumoto R,Takano M

更新日期：2015-08-01 00:00:00

abstract：:After intravenous bolus administration of aprindine (AP) to conscious guinea pigs, the semilogarithmic plasma concentration versus time curve was linear at a dose of 2 mg/kg, but convex at doses of 5 and 10 mg/kg. AP concentrations immediately after administration (C(p0)) were almost identical, irrespective of the dos...

journal_title：Drug metabolism and pharmacokinetics

authors： Shimizu M,Ohota T,Kishida M,Ogata H

更新日期：2002-01-01 00:00:00

abstract：:Decitabine (DAC), a DNA methylation inhibitor, is transported into cancer cells mainly via equilibrative nucleoside transporter 1 (ENT1) and subsequently phosphorylated by deoxycytidine kinase (dCK). We previously reported that apparent DAC uptake into cells may be described using a simple compartment model with clear...

journal_title：Drug metabolism and pharmacokinetics

authors： Ueda K,Nakamura T,Tanaka S,Hosokawa M,Iwakawa S,Ogawara KI

更新日期：2020-02-01 00:00:00

abstract：:Polymorphic human flavin-containing monooxygenase (FMO) 3 is an important drug-metabolizing enzyme for nitrogen- or sulfur-containing compounds. Cynomolgus macaques, a non-human primate species widely used in drug metabolism studies, have corresponding FMO3 molecular and enzymatic similarities to humans; however, gene...

journal_title：Drug metabolism and pharmacokinetics

authors： Uno Y,Shimizu M,Yoda H,Origuchi Y,Yamazaki H

更新日期：2019-02-01 00:00:00

abstract：:The objectives of this study were to evaluate the relative contribution of the direct pathway in overall brain transport for 17 model drugs with different physicochemical properties after nasal administrations and to identify factors that govern the fraction of the dose transported to the brain via the direct pathway ...

journal_title：Drug metabolism and pharmacokinetics

authors： Lee KR,Maeng HJ,Chae JB,Chong S,Kim DD,Shim CK,Chung SJ

更新日期：2010-01-01 00:00:00

abstract：:To evaluate the effect of protein binding of pilsicainide on its clearance and the contribution of protein binding to optimized pilsicainide therapy, clinical laboratory and pharmacokinetic data were studied in 160 Japanese inpatients (Study 1) and 18 Japanese inpatients (Study 2). To determine the relation between pr...

journal_title：Drug metabolism and pharmacokinetics

authors： Fukumoto K,Tanemura M,Tsuchishita Y,Kusumoto M,Matsumoto K,Kamakura S,Ueno K

更新日期：2005-06-01 00:00:00

abstract：:The enzyme activities of CYP2D6 and CYP2C19 show a genetic polymorphism, and the frequency of poor metabolizers (PMs) on these enzymes depends on races. We have analyzed frequencies of mutant alleles and PMs based on the published data in previous study (Shimizu, T. et al.: Bioinformatics research on inter-racial diff...

journal_title：Drug metabolism and pharmacokinetics

authors： Shimizu T,Ochiai H,Asell F,Yokono Y,Kikuchi Y,Nitta M,Hama Y,Yamaguchi S,Hashimoto M,Taki K,Nakata K,Aida Y,Ohashi A,Ozawa N

更新日期：2003-01-01 00:00:00

abstract：:Microdose (MD) clinical trials have been introduced to obtain human pharmacokinetic data early in drug development. Here we assessed the cost-effectiveness of microdose integrated drug development in a hypothetical model, as there was no such quantitative research that weighed the additional effectiveness against the ...

journal_title：Drug metabolism and pharmacokinetics

authors： Yamane N,Igarashi A,Kusama M,Maeda K,Ikeda T,Sugiyama Y

更新日期：2013-01-01 00:00:00

abstract：:Nevirapine (NVP) is widely used as a non-nucleoside reverse transcriptase inhibitor of HIV-1, however, it is associated with severe skin and liver injury. The mechanisms of these adverse reactions are not yet clear, but the metabolic activation of NVP is thought to be related to the injury process. Until now, several ...

journal_title：Drug metabolism and pharmacokinetics

authors： Tateishi Y,Ohe T,Yasuda D,Takahashi K,Nakamura S,Kazuki Y,Mashino T

更新日期：2020-04-01 00:00:00

abstract：:Accumulating evidences have shown that diabetes is often accompanied with depression, thus it is possible that oral antidiabetic agent glyburide and antidepressive agent paroxetine are co-administered in diabetic patients. The aim of this study was to assess interactions between glyburide and paroxetine in rats. Effec...

journal_title：Drug metabolism and pharmacokinetics

authors： Jiang S,Zhao W,Chen Y,Zhong Z,Zhang M,Li F,Xu P,Zhao K,Li Y,Liu L,Liu X

更新日期：2015-06-01 00:00:00

abstract：:The effect of carrageenan-induced acute peripheral inflammation (API) on the pharmacokinetics of the hepatically metabolizing compound midazolam (MDZ) was investigated in rats. Rats were subcutaneously treated with λ-carrageenan in the hind paw to induce API. When MDZ was intravenously administered in male rats, it wa...

journal_title：Drug metabolism and pharmacokinetics

authors： Kajikawa N,Doi M,Kusaba J,Aiba T

更新日期：2014-01-01 00:00:00

abstract：:It has been reported that inhibition of the P-glycoprotein (P-gp) results in the improved absorption of P-gp substrate in the intestinal tract. In fact, the increased permeability of P-gp substrate across the intestinal epithelium was observed following inhibition of P-gp in in vitro experiments. To develop the formul...

journal_title：Drug metabolism and pharmacokinetics

authors： Iida A,Tomita M,Hayashi M

更新日期：2005-04-01 00:00:00

abstract：:UDP-glucuronosyltransferases (UGTs) are drug-metabolizing enzymes essential for the metabolism of endogenous substrates and xenobiotics. The cynomolgus macaque is a nonhuman primate species widely used in drug metabolism studies. The molecular characteristics of UGTs have been extensively investigated in humans, but t...

journal_title：Drug metabolism and pharmacokinetics

authors： Uno Y,Yamazaki H

更新日期：2020-08-01 00:00:00

abstract：:Drug metabolizing activities of cytochromes P450 (P450s, or CYPs) 3A4 and 3A5 in liver microsomes from the cynomolgus monkey [Macaca fascicularis (mf)] were investigated and compared with those of human P450 3A enzymes. Low activities for dealkylation of ethoxyresorufin and pentoxyresorufin were seen in recombinant mo...

journal_title：Drug metabolism and pharmacokinetics

authors： Iwasaki K,Murayama N,Koizumi R,Uno Y,Yamazaki H

更新日期：2010-01-01 00:00:00

abstract：:In a clinical setting, changes in pharmacokinetics due to drug-drug interactions can often directly affect the therapeutic safety and efficacy of drugs. Recently, interest has been shown in drug-drug interactions in the intestine. It is now recognized that changes in the functions of drug transporters substantially in...

journal_title：Drug metabolism and pharmacokinetics

authors： Segawa M,Ogura J,Seki S,Itagaki S,Takahashi N,Kobayashi M,Hirano T,Yamaguchi H,Iseki K

更新日期：2013-01-01 00:00:00

abstract：:OCTN1/SLC22A4 is expressed on apical membranes of small intestine, and is involved in gastrointestinal absorption of its substrates, including the food-derived antioxidant ergothioneine (ERGO). ERGO concentration in circulating blood of patients with inflammatory bowel disease (Crohn's disease) is lower than that in h...

journal_title：Drug metabolism and pharmacokinetics

authors： Shimizu T,Masuo Y,Takahashi S,Nakamichi N,Kato Y

更新日期：2015-06-01 00:00:00

abstract：:  Human cytochrome P450 CYP2A6 and CYP2A13 catalyze nicotine metabolisms and mediate activation of tobacco-specific carcinogens including 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL). In this study, we found rhinacanthins A, B, and C isolated from Rhinac...

journal_title：Drug metabolism and pharmacokinetics

authors： Pouyfung P,Prasopthum A,Sarapusit S,Srisook E,Rongnoparut P

更新日期：2014-01-01 00:00:00

abstract：:The current EMA drug interaction guideline was published in 2012. This guideline gives important recommendations on the information required to elucidate the interaction potential of an investigational drug, both as effects of the investigational drug on the PK of other drugs and effects of other medicinal products on...

journal_title：Drug metabolism and pharmacokinetics

authors： Cole S,Kerwash E,Andersson A

更新日期：2020-02-01 00:00:00

abstract：:Genetic factors have a significant impact on the PK variability of EFV, much higher than other non-genetic factors, such as demography. In this work we have performed a comprehensive PG analysis of genes encoding the major metabolizing enzymes and transporters of EFV, establishing a clear relationship between the PK p...

journal_title：Drug metabolism and pharmacokinetics

authors： Sánchez-Martín A,Cabrera Figueroa S,Cruz R,Porras-Hurtado L,Calvo-Boyero F,Rasool M,Tormes Team.,Domínguez-Gil Hurlé A,Carracedo A

更新日期：2016-10-01 00:00:00

abstract：:To characterize the renal handling of CS-023 (RO4908463), a novel parenteral carbapenem antibiotic, and meropenem in humans, we examined their affinities as substrates to human renal transporters. In vitro studies on the uptake of [14C]CS-023 and [14C]meropenem were conducted using HEK293 cells expressing human organi...

journal_title：Drug metabolism and pharmacokinetics

authors： Shibayama T,Sugiyama D,Kamiyama E,Tokui T,Hirota T,Ikeda T

更新日期：2007-02-25 00:00:00

abstract：:1. Assay methods to detect drug interaction in toxicological samples were established by determining cytochrome P450 content and its activity in liver samples. The O-dealkylation reaction of 7-alkoxycoumarin was indicated to reflect changes in the molecular forms of P450s, and the enzyme induction or inhibition in the...

journal_title：Drug metabolism and pharmacokinetics

authors： Matsubara T

更新日期：2002-01-01 00:00:00

abstract：:New SRM (selected reaction monitoring) data dependent exclusion (MS)(n) measurement makes it possible to obtain MS(3) fragmentation data for all MS(2) fragments, useful for structural determination of drug metabolites using ESI ion trap. MS(2) fragments are produced by cleavage of all protonated molecules at the lone ...

journal_title：Drug metabolism and pharmacokinetics

authors： Tozuka Z,Kaneko H,Shiraga T,Beppu M,Niwa T,Kawamura A,Kagayama A

更新日期：2003-01-01 00:00:00

abstract：:Protein kinases are potential drug targets for the treatment of a variety of diseases, including cancer. In particular, specific tyrosine kinase inhibitors are rapidly being developed as new drugs for the inhibition of malignant cell growth and metastasis formation. Most of these newly developed tyrosine kinase inhibi...

journal_title：Drug metabolism and pharmacokinetics

authors： Saito H,An R,Hirano H,Ishikawa T

更新日期：2010-01-01 00:00:00

abstract：:We discovered a novel single nucleotide polymorphism (SNP) at position 325 (G325A) in exon 5 of the multidrug-resistance 1 (MDR1) gene in a study of 37 healthy Japanese subjects. Details are as follows. SNP, 020614Honda001; GENE NAME, human P-glycoprotein (MDR1); ACCESSION NUMBER, M29427; LENGTH, 25 bases; 5'-ATGAATCT...

journal_title：Drug metabolism and pharmacokinetics

authors： Honda T,Dan Y,Koyabu N,Ieiri I,Otsubo K,Higuchi S,Ohtani H,Sawada Y

更新日期：2002-01-01 00:00:00