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Drug Metabolism and Disposition Fast Forward
First published on September 20, 2005; DOI: 10.1124/dmd.105.005264

0090-9556/05/3312-1845-1851$20.00
DMD 33:1845-1851, 2005

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FUNCTIONAL CHARACTERIZATION OF HUMAN MONOCARBOXYLATE TRANSPORTER 6 (SLC16A5)

Yuichi Murakami, Noriko Kohyama, Yasuna Kobayashi, Masayuki Ohbayashi, Hisakazu Ohtani, Yasufumi Sawada, and Toshinori Yamamoto

Department of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University, Tokyo, Japan (Y.M., N.K., Y.K., M.O., T.Y.); Department of Medico-Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan (Y.M., H.O.); and Laboratory of Drug Informatics, Graduate School of Pharmaceutical Sciences, the University of Tokyo, Tokyo, Japan (Y.S.)

Human monocarboxylate transporter 6 (MCT6) has recently been isolated, and its tissue distribution has been established at the mRNA level, but its functional properties remain unknown. The aim of this study is to investigate the transport properties of MCT6. When expressed in Xenopus laevis oocytes, MCT6 transported [3H]bumetanide in a pH- and membrane potential-sensitive but not proton gradient-dependent manner, with the Kt value of 84 µM. Furthermore, MCT6 transported various drugs such as probenecid and nateglinide. Neither [14C]L-lactic acid nor [3H]L-tryptophan, typical substrates of other MCT isoforms, was transported by MCT6. Four loop diuretics, i.e., furosemide, piretanide, azosemide, and torasemide, thiazides, probenecid, glibenclamide, and nateglinide inhibited the MCT6-mediated uptake of [3H]bumetanide. In contrast, short-chain carboxylic acids, such as L-lactic acid and succinic acid did not inhibit the MCT6-mediated uptake of bumetanide. These results suggest that the substrate specificity of MCT6 is distinct from those of other MCTs. Bumetanide would be a good tool for investigating the functional properties of MCT6. It is probable that MCT6 is involved in the disposition of various drugs, including bumetanide.

Address correspondence to: Dr. Toshinori Yamamoto, Department of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan. E-mail: yamagen{at}pharm.showa-u.ac.jp




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