6-Hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor elevated in renal failure patients.

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：:UDP-glucuronosyltransferases (UGTs) catalyze the glucuronidation of a wide variety of xeno/endobiotics. Previous studies have reported that human UGT enzymes are phosphorylated and that treatment of cells with protein kinase C (PKC) inhibitors results in decreased UGT activities without affecting the UGT protein level...

journal_title：Drug metabolism and pharmacokinetics

authors： Abe Y,Fujiwara R,Oda S,Yokoi T,Nakajima M

更新日期：2011-06-01 00:00:00

abstract：:It is now widely appreciated that drug metabolites, in addition to the parent drugs themselves, can mediate the serious adverse effects exhibited by some new therapeutic agents, and as a result, there has been heightened interest in the field of drug metabolism from researchers in academia, the pharmaceutical industry...

journal_title：Drug metabolism and pharmacokinetics

authors： Baillie TA,Rettie AE

更新日期：2011-01-01 00:00:00

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：: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：:The HCT-15 human colon cancer cell line has a Na(+)-dependent carrier-mediated transport system for the uptake of glycerol. A similar transport system has been suggested to be present also in the small intestine and is of interest with regard to its role in the absorption of glycerol and possibly some structurally rel...

journal_title：Drug metabolism and pharmacokinetics

authors： Fujimoto N,Inoue K,Ohgusu Y,Hayashi Y,Yuasa H

更新日期：2007-06-01 00:00:00

abstract：:Maleic acid (MA) was purposefully adulterated in an array of starch-based foods in Taiwan, inciting a food safety incident. Due to limited data on the pharmacokinetics and bioavailability of ingested MA, we studied pharmacokinetic (PK) parameters in serum and urine of Sprague Dawley rats. Three groups of male and fema...

journal_title：Drug metabolism and pharmacokinetics

authors： Wu C,Chen HC,Luo YS,Chiang SY,Wu KY

更新日期：2016-12-01 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：: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

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 and cynomolgus macaque flavin-containing monooxygenases (FMO) 3 are important oxygenation enzymes for nitrogen-containing drugs. Inter-animal variability of FMO3-dependent drug oxygenations in vivo is suspected in cynomolgus macaques because such variability is evident in humans. Therefore, this foll...

journal_title：Drug metabolism and pharmacokinetics

authors： Shimizu M,Uno Y,Utoh M,Yamazaki H

更新日期：2020-12-01 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：: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：:The ATP-binding cassette transporter, ABCG2, which is expressed at high levels in the intestine and liver, functions as an efflux transporter for many drugs, including clinically used anticancer agents such as topotecan and the active metabolite of irinotecan (SN-38). In this study, to elucidate the linkage disequilib...

journal_title：Drug metabolism and pharmacokinetics

authors： Maekawa K,Itoda M,Sai K,Saito Y,Kaniwa N,Shirao K,Hamaguchi T,Kunitoh H,Yamamoto N,Tamura T,Minami H,Kubota K,Ohtsu A,Yoshida T,Saijo N,Kamatani N,Ozawa S,Sawada J

更新日期：2006-04-01 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：: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：:Medication therapy is the first line of treatment in the management of epilepsy. Fetal exposure to valproic acid (VPA), an antiepileptic drug, poses an elevated risk of teratogenicity in early pregnancy. Some studies have reported that monocarboxylate transporters (MCTs) may be involved in the placental transport of V...

journal_title：Drug metabolism and pharmacokinetics

authors： Ishiguro Y,Furugen A,Narumi K,Nishimura A,Hirano T,Kobayashi M,Iseki K

更新日期：2018-12-01 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：: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：: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：:  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：: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：UNLABELLED:Better prediction of drug disposition prior to the clinical trial is critical for the efficient development of new drugs. The purpose of this study is to develop a novel multiple assessment methodology of hepatocellular drug disposition from drug uptake to efflux including biliary and basolateral excretion, ...

journal_title：Drug metabolism and pharmacokinetics

authors： Takahashi R,Ichikawa H,Kanda K

更新日期：2016-04-01 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：:Repeated pretreatment with the antimalarial drug artemisinin (QHS) could lead to reduced exposure to the parent drug, which is mainly mediated by auto-induction of CYP2B6 activity. CYP2B6 is most sensitive to the inductive effect of constitutive androstane receptor (CAR), which can be activated by QHS. CYP2B6 polymorp...

journal_title：Drug metabolism and pharmacokinetics

authors： Zang M,Zhao L,Zhu F,Li X,Yang A,Xing J

更新日期：2015-02-01 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：:Thirty-nine genetic variations, including thirty novel ones, were found in the human SLC29A1 gene, which encodes equilibrative nucleoside transporter 1, from 256 Japanese cancer patients administered gemcitabine. The found novel variations included -8,166G>A, -81,10A>G, -7,947G>A, -7,789T>C, -5,595G>A, -3,803_-3,783de...

journal_title：Drug metabolism and pharmacokinetics

authors： Kim SR,Saito Y,Maekawa K,Sugiyama E,Kaniwa N,Ueno H,Okusaka T,Morizane C,Yamamoto N,Ikeda M,Yoshida T,Minami H,Furuse J,Ishii H,Saijo N,Kamatani N,Ozawa S,Sawada J

更新日期：2006-06-01 00:00:00

abstract：:Tralokinumab is a human monoclonal antibody in clinical development for asthma and atopic dermatitis that specifically neutralizes interleukin-13. This phase I, single-blind, randomized, placebo-controlled, single ascending-dose study assessed the safety, tolerability, pharmacokinetics (PK), and immunogenicity of subc...

journal_title：Drug metabolism and pharmacokinetics

authors： Baverel P,She D,Piper E,Ueda S,Yoshioka T,Faggioni R,Gevorkyan H

更新日期：2018-06-01 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：: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