Trimethylamine N-oxygenation in cynomolgus macaques genotyped for flavin-containing monooxygenase 3 (FMO3).

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：: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：:Morphine is one of the strongest analgesics and is commonly used for the treatment of chronic pain. The pharmacokinetic properties of morphine are, in part, modulated by P-glycoprotein (P-gp). We previously reported that intestinal P-gp expression levels are influenced via the activation of inducible nitric oxide synt...

journal_title：Drug metabolism and pharmacokinetics

authors： Nawa A,Fujita-Hamabe W,Kishioka S,Tokuyama S

更新日期：2011-01-01 00:00:00

abstract：:The interaction between cytochrome P450s (CYP, P450) and UDP-glucuronosyltransferases (UGTs) was studied by co-immunoprecipitation. P450 isoform-selective antibody was used as a probe to co-precipitate UGTs with the P450s from solubilized rat liver microsomes. Antibodies toward CYP3A2, CYP2B2, CYP2C11/13 and CYP1A2 co...

journal_title：Drug metabolism and pharmacokinetics

authors： Ishii Y,Iwanaga M,Nishimura Y,Takeda S,Ikushiro S,Nagata K,Yamazoe Y,Mackenzie PI,Yamada H

更新日期：2007-10-01 00:00:00

abstract：:The mRNA levels of human cytochrome P450 (CYP)2Cs and CYP3As in primary cultures of freshly isolated human hepatocytes were assessed after exposure to NO-1886 and rifampicin, a typical inducer of CYP3As. mRNA levels were analyzed by real-time RT-PCR using an ABI PRISM 7700 Sequence Detector system. Exposure to NO-1886...

journal_title：Drug metabolism and pharmacokinetics

authors： Morioka Y,Nishimura M,Imai T,Suzuki S,Harada M,Satoh T,Naito S

更新日期：2006-02-01 00:00:00

abstract：:To investigate the transport function of the blood-brain barrier (BBB), we employed an in vitro model of the BBB, consisting of a co-culture of porcine brain capillary endothelial cells (BCECs) with rat astrocytes. Porcine BCECs were cultured on a filter insert with rat astrocytes on the underlying plastic well. Rat a...

journal_title：Drug metabolism and pharmacokinetics

authors： Kido Y,Tamai I,Nakanishi T,Kagami T,Hirosawa I,Sai Y,Tsuji A

更新日期：2002-01-01 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：:The present study aims is to investigate the metabolic mechanism of Xue-Fu-Zhu-Yu decoction (XFZYD) in the treatment of blood-stasis syndrome in Coronary Heart Disease (CHD). To that end, 30 CHD patients with Blood-Stasis Syndrome (BSS) and 20 healthy subjects were enrolled. LC-Q-TOF/MS analysis determined that in com...

journal_title：Drug metabolism and pharmacokinetics

authors： Yi M,Li Q,Zhao Y,Nie S,Wu N,Wang D

更新日期：2019-10-01 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 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：:In the present study, we identified three novel single nucleotide polymorphisms (SNPs), 147C>T in exon 2 (silent), 602G>C in exon 3 (Arg201Pro), and 1134C>T in exon 4 (silent), in the gene of bile acid CoA: amino acid N-acyltransferase (BAAT) by resequencing the entire coding region and the exon-intron junctions of 10...

journal_title：Drug metabolism and pharmacokinetics

authors： Tougou K,Fukuda T,Ito T,Yamazaki H,Fujio Y,Azuma J

更新日期：2007-04-01 00:00:00

abstract：:Guanfacine hydrochloride extended-release tablet (GXR) is approved for child and adolescent patients with attention-deficit/hyperactivity disorder (ADHD). The aims of this study were to develop a population pharmacokinetic model of guanfacine after administration of GXR and to evaluate factors influencing the pharmaco...

journal_title：Drug metabolism and pharmacokinetics

authors： Tsuda Y,Matsuo Y,Matsumoto S,Wajima T

更新日期：2019-12-01 00:00:00

abstract：:The object of this analysis was to develop a population pharmacokinetic model of micafungin, a new anti-fungal agent of the echinocandin class, to optimize dosing in Japanese patients with fungal infections. Population pharmacokinetics parameters were determined using NONMEM based on pharmacokinetic data from 198 subj...

journal_title：Drug metabolism and pharmacokinetics

authors： Tabata K,Katashima M,Kawamura A,Kaibara A,Tanigawara Y

更新日期：2006-08-01 00:00:00

abstract：:The objectives of this study were to develop a population pharmacokinetic model of imidafenacin and to explore the factors that affect the pharmacokinetics of imidafenecin. A total of 2406 plasma samples were collected from 90 healthy volunteers and 457 patients with overactive bladder. We determined the plasma concen...

journal_title：Drug metabolism and pharmacokinetics

authors： Ohno T,Nakade S,Nakayama K,Kitagawa J,Miyabe H,Konomi T,Miyata Y

更新日期：2008-01-01 00:00:00

abstract：:A population pharmacokinetic (PK) model for meropenem in Japanese pediatric patients with various infectious diseases was developed based on 116 plasma concentrations from 50 pediatric patients. The population PK parameters developed in this analysis are useful for calculation of the percent time above minimum inhibit...

journal_title：Drug metabolism and pharmacokinetics

authors： Ohata Y,Tomita Y,Nakayama M,Kozuki T,Sunakawa K,Tanigawara Y

更新日期：2011-01-01 00:00:00

abstract：:Hypoglycemia is one of the serious adverse effects induced by cibenzoline (CBZ), an antiarrhythmic agent. In order to clarify the pharmacodynamics of CBZ-induced hypoglycemia, CBZ was administered intravenously to conscious rats at a dose of 5, 10 or 20 mg/kg and serum samples were collected periodically to determine ...

journal_title：Drug metabolism and pharmacokinetics

authors： Takahashi Y,Ishiwata Y,Kojima Y,Yasuhara M

更新日期：2011-06-01 00:00:00

abstract：SUMMARY:The diagnosis of cardiac ischemia remains a challenge in contemporary emergency medicine. A blood-borne biomarker is an attractive alternative to cardiac imaging or stress testing as it would be cheaper and logistically faster to obtain. A number of candidate biomarkers have been proposed for the detection of c...

journal_title：Drug metabolism and pharmacokinetics

authors： Gaze DC

更新日期：2009-01-01 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：:Prothrombin time (PT) has been widely used for measuring anticoagulation intensity under rivaroxaban therapy, but precise information has not been well established yet. Consecutive 96 non-valvular atrial fibrillation (NVAF) under rivaroxaban between Jan/June, 2015 were recruited. Serum concentration (SC) and PT with 5...

journal_title：Drug metabolism and pharmacokinetics

authors： Suzuki S,Yamashita T,Kasai H,Otsuka T,Sagara K

更新日期：2018-08-01 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：:Clinical studies have revealed that some fluoroquinolones may cause severe adverse effects when co-administered with substrates of CYP1A2. Our previous study showed antofloxacin (ATFX) was responsible for mechanism-based inhibition (MBI) of the metabolism of phenacetin in rats. In the clinical setting, ATFX is likely ...

journal_title：Drug metabolism and pharmacokinetics

authors： Pan X,Wang P,Hu N,Liu L,Liu X,Xie L,Wang G

更新日期：2011-01-01 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：: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：: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：:The roots of Sophora flavescens (Sf) have been widely used as a herbal medicine for the treatment of diarrhea, gastrointestinal hemorrhage, and eczema. Cytochrome P450 (P450) forms including CYP1A2, CYP2B, CYP2E1, and CYP3A participate in the oxidative metabolism of theophylline, which is an important bronchodilation ...

journal_title：Drug metabolism and pharmacokinetics

authors： Ueng YF,Tsai CC,Lo WS,Yun CH

更新日期：2010-01-01 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：:Eight covalent tyrosine kinase inhibitors (TKIs) were investigated to determine the characteristics of their covalent binding to plasma proteins. The data revealed that their covalent binding to plasma proteins is of species difference. In addition to the reports on neratinib and pyrotinib, osimertinib, alflutinib, AS...

journal_title：Drug metabolism and pharmacokinetics

authors： Liu X,Feng D,Zheng M,Cui Y,Zhong D

更新日期：2020-10-01 00:00:00

abstract：:Most of cytochrome P450 (CYP) expressions are regulated by nuclear receptors. The regulation pathways of transcription are activated by binding of the ligand to the receptor. Many combination of CYPs and nuclear receptors in transcriptional regulation have been reported. However, we have reported that the combination ...

journal_title：Drug metabolism and pharmacokinetics

authors： Terashima J,Jimma Y,Jimma K,Hakata S,Yachi M,Habano W,Ozawa S

更新日期：2018-08-01 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：:Resistance to antiemetic treatment with 5-hydroxytryptamine 3 receptor antagonists is a problem, with 20-30% of patients showing unsatisfactory responses. Efflux transport by P-glycoprotein, encoded by the ATP-binding cassette ABCB1 gene in the blood-brain barrier, has been the suggested resistance mechanism. We evalu...

journal_title：Drug metabolism and pharmacokinetics

authors： Tsuji D,Kim YI,Nakamichi H,Daimon T,Suwa K,Iwabe Y,Hayashi H,Inoue K,Yoshida M,Itoh K

更新日期：2013-01-01 00:00:00