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Vol. 30, Issue 2, 220-223, February 2002

Effect of 17beta -Estradiol-D-17beta -Glucuronide on the Rat Organic Anion Transporting Polypeptide 2-Mediated Transport Differs Depending on Substrates

Daisuke Sugiyama, Hiroyuki Kusuhara, Yoshihisa Shitara, Takaaki Abe, and Yuichi Sugiyama

Graduate School of Pharmaceutical Sciences, the University of Tokyo, Bunkyo-ku, Tokyo, Japan (D.S., H.K., Y.Su.); School of Pharmaceutical Sciences, Kitasato University, Minato-ku, Tokyo, Japan (Y.Sh.); Department of Neurophysiology, 1st Department of Surgery, Tohoku University School of Medicine, Sendai, Japan (T.A.)

Rat organic anion transporting polypeptide 2 (rOatp2) is a member of the OATP family. It exhibits broad substrate specificity and accepts amphipathic organic anions, cardiac glycosides (digoxin and ouabain; a neutral compound), and organic cations (rocuronium and N-(4,4-azo-n-pentyl)-21-deoxyajamalinium). In the present study, kinetic analyses were carried out to investigate whether taurocholate (TCA), digoxin, and 17beta -estradiol-D-17beta -glucuronide (E217beta G) share the same recognition site on rOatp2 for their transport. The transport of TCA and digoxin was mutually inhibited, and the Ki values of digoxin and TCA for the transport of TCA and digoxin were 0.58 and 160 µM, respectively. The Km and Vmax values of TCA and digoxin were 190 µM and 140 pmol/min/mg of protein and 1.1 µM and 6.6 pmol/min/mg of protein, respectively. The Km and Ki values were consistent. In addition, digoxin (1 µM) and TCA (100 µM) increased the Km values of TCA and digoxin, respectively, but they did not affect the Vmax values, suggesting that their inhibition is competitive. The transport of digoxin via rOatp2 was inhibited slightly by E217beta G, whereas the uptake of TCA was stimulated by E217beta G in a concentration-dependent manner. These results suggest that rOatp2 has at least two substrate recognition sites, one for TCA and digoxin and the other for E217beta G.

Copyright © 2002 by The American Society for Pharmacology and Experimental Therapeutics


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Copyright © 2002 by the American Society for Pharmacology and Experimental Therapeutics.