Genetic polymorphism of bile acid CoA: amino acid N-acyltransferase in Japanese individuals.

abstract：:Twenty genetic variations, including seven novel ones, were found in the human SLC22A1 gene, which encodes organic cation transporter 1, from 116 Japanese individuals. The novel variations were as follows: -94C>A in the 5'-untranslated region (A of the translation start codon is numbered +1 in the cDNA sequence; MPJ6_...

journal_title：Drug metabolism and pharmacokinetics

authors： Itoda M,Saito Y,Maekawa K,Hichiya H,Komamura K,Kamakura S,Kitakaze M,Tomoike H,Ueno K,Ozawa S,Sawada J

更新日期：2004-08-01 00:00:00

abstract：:Most cephalosporin antibiotics are excreted into urine via glomerular filtration and active tubular secretion by renal organic anion transporters. In this study, we investigated the interaction of cephalosporins with rat organic anion transporter rOAT1, mainly expressed at the basolateral membrane of the renal proxima...

journal_title：Drug metabolism and pharmacokinetics

authors： Uwai Y,Saito H,Inui K

更新日期：2002-01-01 00:00:00

abstract：:Oligopeptide transporter PEPT1 is thought to be involved in the intestinal absorption and renal reabsorption of peptides and therapeutic agents. The driving force of PEPT1 is H+ gradient, a part of which is supplied by Na+/H+ exchanger (NHE) expressed on the apical surface of the epithelium although molecular identifi...

journal_title：Drug metabolism and pharmacokinetics

authors： Watanabe C,Kato Y,Ito S,Kubo Y,Sai Y,Tsuji A

更新日期：2005-12-01 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 hepatic uptake transporter organic anion transporting polypeptide (OATP) 1B1 is inhibited by some uremic toxins; however, direct inhibition can only partially explain the delayed systemic elimination of substrate drugs in renal failure patients. This study aimed to examine the long-lasting inhibition of OATP1B1 by...

journal_title：Drug metabolism and pharmacokinetics

authors： Masuo Y,Fujita KI,Mishiro K,Seba N,Kogi T,Okumura H,Matsumoto N,Kunishima M,Kato Y

更新日期：2020-12-01 00:00:00

abstract：:Cytochrome P450 (P450) constitutes a superfamily of enzymes which activate dioxygen and carry out monooxygenation reactions of large numbers of endogenous and xenobiotic compounds. Drug metabolism is a particularly important P450 function, and, therefore, elucidating the metabolic products and pathways of drugs is ess...

journal_title：Drug metabolism and pharmacokinetics

authors： Yasui H,Hayashi S,Sakurai H

更新日期：2005-02-01 00:00:00

abstract：:The purpose of the present study was to evaluate and compare the absolute protein expression levels of 28 drug-related transporters in Caco-2 cell monolayers cultured for 2, 3, and 4 weeks. Plasma membrane fractions of Caco-2 cells cultured on Transwell inserts for 2, 3 and 4 weeks were prepared and digested with tryp...

journal_title：Drug metabolism and pharmacokinetics

authors： Uchida Y,Ohtsuki S,Kamiie J,Ohmine K,Iwase R,Terasaki T

更新日期：2015-04-01 00:00:00

abstract：:Human carboxylesterase 1 (hCE-1, CES1A1, HU1) and carboxylesterase 2 (hCE-2, hiCE, HU3) are a serine esterase involved in both drug metabolism and activation. Although both hCE-1 and hCE-2 are present in several organs, the hydrolase activity of liver and small intestine is predominantly attributed to hCE-1 and hCE-2,...

journal_title：Drug metabolism and pharmacokinetics

authors： Imai T

更新日期：2006-06-01 00:00:00

abstract：:The injectable form of oxycodone contains hydrocotarnine that is supposed to potentiate the analgesic effect of oxycodone with unknown mechanism(s). In this study, the effects of hydrocotarnine on the cytochrome P450 (CYP) and P-glycoprotein (P-gp) were investigated. Hydrocotarnine did not induce a significant change ...

journal_title：Drug metabolism and pharmacokinetics

authors： Ito K,Kubota Y,Toda T,Suto S,Ikarashi N,Sugiyama K

更新日期：2009-01-01 00:00:00

abstract：:The drug interaction between new quinolone antibiotics (NQs) and polyvalent metal cation products, leading to a significant decrease in the absorption of NQ, is considered to be attributable to the formation of poorly absorbable chelate and physicochemical adsorption of NQs to cation products. To clarify the mechanism...

journal_title：Drug metabolism and pharmacokinetics

authors： Imaoka A,Hattori M,Akiyoshi T,Ohtani H

更新日期：2014-01-01 00:00:00

abstract：:Genetic polymorphisms in xenobiotic transporters have recently been clarified to be associated with change in drug distribution and disposition. To expand on recent identification of direct interaction and functional regulation of several transporters by a PDZ (PSD95, Dlg and ZO1) domain containing protein PDZK1, the ...

journal_title：Drug metabolism and pharmacokinetics

authors： Sugiura T,Kato Y,Kubo Y,Tsuji A

更新日期：2006-10-01 00:00:00

abstract：:Dihydrofolate reductase gene (DHFR) 19-bp deletion polymorphisms result in varied DHFR enzymatic activity affecting the risk for preterm delivery, spina bifida, and the efficacy of methotrexate (MTX). Ethnic differences in DHFR 19-bp polymorphisms may be responsible for the divergent findings in previous genetic studi...

journal_title：Drug metabolism and pharmacokinetics

authors： Hayashi H,Horino M,Morishita M,Tazoe Y,Tsuboi S,Matsuyama T,Kosuge K,Yamada H,Tsuji D,Inoue K,Itoh K

更新日期：2010-01-01 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：: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：: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：:Altered expression of P-glycoprotein (P-gp), a drug efflux transporter expressed by brain capillary endothelial cells (BCECs), may contribute to the development of opioid analgesic tolerance, as demonstrated by cumulative evidence from research. However, the detailed mechanism by which chronic morphine treatment incre...

journal_title：Drug metabolism and pharmacokinetics

authors： Kobori T,Fujiwara S,Miyagi K,Harada S,Nakamoto K,Nakagawa T,Takahashi H,Narita M,Tokuyama S

更新日期：2014-01-01 00:00:00

abstract：:A population pharmacokinetic substudy design of a new chemical entity was evaluated based on the bias in parameter estimates and the power of detecting a specific subpopulation showing different clearance using a clinical trial simulation approach. The effect of analysis algorithms on type I error was also assessed. T...

journal_title：Drug metabolism and pharmacokinetics

authors： Nakade S,Nishibori A,Okamoto H,Higuchi S

更新日期：2004-10-01 00:00:00

abstract：:Pregnane X receptor (PXR) is a ligand-activated nuclear factor that upregulates the expression of proteins involved in the detoxification and clearance of xenobiotics, primarily cytochrome P450 3A4 (CYP3A4). Structure-activity relationship (SAR) analysis of PXR agonists is useful for avoiding unwanted pharmacokinetics...

journal_title：Drug metabolism and pharmacokinetics

authors： Yoshida S,Yamashita F,Itoh T,Hashida M

更新日期：2012-01-01 00:00:00

abstract：:In this study, a simple in vitro method for detecting human P450 (CYP) quasi-irreversible and irreversible inhibitors was evaluated. For the method, cDNA-expressed CYPs were applied to microtiter plate assays, CYP inhibitors were co-incubated with fluorometric substrates, and IC(50) were continuously measured (without...

journal_title：Drug metabolism and pharmacokinetics

authors： Naritomi Y,Teramura Y,Terashita S,Kagayama A

更新日期：2004-02-01 00:00:00

abstract：:In drug discovery, the cerebrospinal fluid (CSF) drug concentration (CCSF) has been used as a surrogate for the interstitial fluid (ISF) concentration (CISF). However, the CCSF-to-CISF gradient suggested for P-glycoprotein (P-gp) substrates in rodents causes uncertainty in CISF estimations and subsequent pharmacokinet...

journal_title：Drug metabolism and pharmacokinetics

authors： Nagaya Y,Nozaki Y,Takenaka O,Watari R,Kusano K,Yoshimura T,Kusuhara H

更新日期：2016-02-01 00:00:00

abstract：:CYP2D6 is involved in the biotransformation of a large number of drugs, including risperidone. This study was designed to detect CYP2D6 polymorphisms with a Luminex assay, including assessment the relationship of CYP2D6 polymorphisms and risperidone plasma concentration in autism spectrum disorder children (ASD) treat...

journal_title：Drug metabolism and pharmacokinetics

authors： Vanwong N,Ngamsamut N,Hongkaew Y,Nuntamool N,Puangpetch A,Chamnanphon M,Sinrachatanant A,Limsila P,Sukasem C

更新日期：2016-04-01 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：:Methyl gallate (MG) and pentagalloyl glucopyranose (PGG) are bioactive phenolic compounds that possess various pharmacological activities. However, the knowledge of hepatic metabolism of MG and PGG is limited. The purpose of this study was to investigate the in vitro glucuronidation of MG and PGG using liver microsome...

journal_title：Drug metabolism and pharmacokinetics

authors： Jiamboonsri P,Pithayanukul P,Bavovada R,Leanpolchareanchai J,Gao S,Hu M

更新日期：2016-08-01 00:00:00

abstract：:Forty-eight single nucleotide variations, including 27 novel ones, were found in the 5'- regulatory region, all of the exons and their surrounding introns of CYP2C19 in 253 Japanese subjects (134 diabetic patients and 119 healthy volunteers). Identified novel variations were as follows: -2772G>A, 2767_-2760delGGTGAACA...

journal_title：Drug metabolism and pharmacokinetics

authors： Fukushima-Uesaka H,Saito Y,Maekawa K,Ozawa S,Hasegawa R,Kajio H,Kuzuya N,Yasuda K,Kawamoto M,Kamatani N,Suzuki K,Yanagawa T,Tohkin M,Sawada J

更新日期：2005-08-01 00:00:00

abstract：:Cytochrome P450 (CYP) 3A-related drug-drug interaction (DDI) studies are needed during drug development to determine clinical interaction effects. We aimed to evaluate DDI between sildenafil and two CYP3A inhibitors, clarithromycin and itraconazole, regarding the changes in pharmacokinetics and endogenous markers. An ...

journal_title：Drug metabolism and pharmacokinetics

authors： Lee S,Kim AH,Yoon S,Lee J,Lee Y,Ji SC,Yoon SH,Lee S,Yu KS,Jang IJ,Cho JY

更新日期：2021-02-01 00:00:00

abstract：:The aim of this study was to investigate the impact of genetic polymorphisms in the metabolic and cellular transport pathway of methotrexate (MTX) on the clinical outcome of MTX monotherapy in Japanese rheumatoid arthritis (RA) patients. Fifty-five patients were treated with MTX monotherapy at a dose of 4-10 mg/week. ...

journal_title：Drug metabolism and pharmacokinetics

authors： Kato T,Hamada A,Mori S,Saito H

更新日期：2012-01-01 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：: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：:Polymorphic distributions of pharmacogenes among some ethnicities are under-represented in current pharmacogenetic research. Particularly, there is a paucity of pharmacogenetic information in the Sherpa population in Tibet. We used the Sequenom MassARRAY single nucleotide polymorphism (SNP) genotyping technology to de...

journal_title：Drug metabolism and pharmacokinetics

authors： Wang L,Ren Y,Shi X,Yuan D,Liu K,Geng T,Li G,Kang L,Jin TB

更新日期：2016-02-01 00:00:00

abstract：:Trimethylaminuria is caused by excessive malodorous trimethylamine excreted via urine and body secretion by decreased hepatic flavin-containing monooxygenase 3 (FMO3) metabolic capacity for transforming non-odorous trimethylamine N-oxide. This study investigates foodstuff first in healthy volunteers for palliative car...

journal_title：Drug metabolism and pharmacokinetics

authors： Shimizu M,Kozono M,Murayama N,Yamazaki H

更新日期：2009-01-01 00:00:00