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Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells.

Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells. Research Abstract Details 

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  • Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells. Abstract Text:

    kenji kuwayamaKenji Kuwayama,hiroyuki inoueHiroyuki Inoue,tatsuyuki kanamoriTatsuyuki Kanamori,kenji tsujikawaKenji Tsujikawa,hajime miyaguchiHajime Miyaguchi,yuko iwataYuko Iwata,seiji miyauchiSeiji Miyauchi,naoki kamoNaoki Kamo,tohru kishiTohru Kishi,

    3,4-Methylenedioxymethamphetamine (MDMA) is an illegal amphetamine-type stimulant (ATS) that is abused orally in the form of tablets for recreational purposes. The aim of this work is to investigate the absorption mechanism of MDMA and other related compounds that often occur together in ATS tablets, and to determine whether such tablet components interact with each other in intestinal absorption. The characteristics of MDMA uptake by the human intestinal epithelial Caco-2 cell line were investigated. The Michaelis constant and the maximal uptake velocity at pH 6.0 were 1.11 mM and 13.79 nmol/min/mg protein, respectively, and the transport was electroneutral. The initial uptake rate was regulated by both intra- and extracellular pH. MDMA permeation from the apical to the basolateral side was inferior to that in the reverse direction, and a decrease in apical pH enhanced MDMA permeation from the basolateral to the apical side. These facts indicate that this transport system may be an antiporter of H(+). However, under physiological conditions, the proton gradient cannot drive the MDMA uptake because it is inwardly directed. Large concentration differences of MDMA itself drive this antiporter. Various compounds with similar amine moieties inhibited the uptake, but substrates of organic cation transporters (OCT1-3) and an H(+)-coupled efflux antiporter, MATE, were not recognized.

    Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells. Publishing Authors By Initials

    k kuwayamaK Kuwayama,h inoueH Inoue,t kanamoriT Kanamori,k tsujikawaK Tsujikawa,h miyaguchiH Miyaguchi,y iwataY Iwata,s miyauchiS Miyauchi,n kamoN Kamo,t kishiT Kishi,

    For similar abstracts research abstracts see: abstracts research

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    Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells. Journal Published:

    PUBLICATION TYPE: Journal Article

    Journal: Biochimica et biophysica acta

    VOLUME: 1778

    Page Numbers: 42-50

    Journal Abbreviation: Biochim. Biophys. Acta

    ISSN: 0006-3002

    DAY: 8

    MONTH: 09

    YEAR: 2007

    Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells. Information

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    LANGUAGE: eng

    NlmUniqueID: 217513

    Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells. Keywords Mesh Terms:

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    Grant and Affiliation Information for Uptake of 3,4-methylenedioxymethamphetamine and its related compounds by a proton-coupled transport system in Caco-2 cells.

    AFFILIATION: National Research Institute of Police Science, 6-3-1, Kashiwanoha, Kashiwa, Chiba 277-0882, Japan; Laboratory of Biophysical Chemistry, Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo 060-0812, Japan.

    Country: Netherlands

    Netherlands Research PublicationNetherlands Research Publication

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    MEDLINETA: Biochim Biophys Acta

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