PT  - JOURNAL ARTICLE
AU  - Yasuna Kobayashi
AU  - Ryoko Sakai
AU  - Naomi Ohshiro
AU  - Masayuki Ohbayashi
AU  - Noriko Kohyama
AU  - Toshinori Yamamoto
TI  - POSSIBLE INVOLVEMENT OF ORGANIC ANION TRANSPORTER 2 ON THE INTERACTION OF THEOPHYLLINE WITH ERYTHROMYCIN IN THE HUMAN LIVER
AID  - 10.1124/dmd.104.003301
DP  - 2005 May 01
TA  - Drug Metabolism and Disposition
PG  - 619--622
VI  - 33
IP  - 5
4099  - http://dmd.aspetjournals.org/content/33/5/619.short
4100  - http://dmd.aspetjournals.org/content/33/5/619.full
SO  - Drug Metab Dispos2005 May 01; 33
AB  - Organic anion transporter 2 (Oat2 [SLC22A7]) is a multispecific organic anion transporter. Although several substrates of human Oat2 (hOat2) have been elucidated, a possible involvement of hOat2 in drug interaction is less defined. The purpose of this study was to investigate the interaction of theophylline with erythromycin mediated by hOat2 using a Xenopus laevis oocyte expression system. When expressed in Xenopus oocytes, hOat2 mediated the transport of theophylline and erythromycin. The finding indicates that the two compounds are novel substrates for hOat2. The apparent Km values for the uptake of hOat2 that mediated the transport of theophylline and erythromycin were 12.6 μM and 18.5 μM, respectively. The hOat2-mediated uptake of [14C]theophylline and [14C]erythromycin was cis-inhibited by adding erythromycin and theophylline, respectively. Our present findings suggest that hOat2 may, at least in part, be involved in the theophylline-erythromycin interaction in the human liver. The American Society for Pharmacology and Experimental Therapeutics