RT Journal Article
SR Electronic
T1 POSSIBLE INVOLVEMENT OF ORGANIC ANION TRANSPORTER 2 ON THE INTERACTION OF THEOPHYLLINE WITH ERYTHROMYCIN IN THE HUMAN LIVER
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 619
OP 622
DO 10.1124/dmd.104.003301
VO 33
IS 5
A1 Yasuna Kobayashi
A1 Ryoko Sakai
A1 Naomi Ohshiro
A1 Masayuki Ohbayashi
A1 Noriko Kohyama
A1 Toshinori Yamamoto
YR 2005
UL http://dmd.aspetjournals.org/content/33/5/619.abstract
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