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Am J Physiol Renal Physiol 281: F454-F468, 2001;
0363-6127/01 $5.00
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Vol. 281, Issue 3, F454-F468, September 2001

Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1

Petra Arndt1,*, Christopher Volk1,*, Valentin Gorboulev1, Thomas Budiman2, Christian Popp1, Isabel Ulzheimer-Teuber1, Aida Akhoundova1, Stefan Koppatz1, Ernst Bamberg2, Georg Nagel2, and Hermann Koepsell1

1 Institute of Anatomy of the Bayerische Julius-Maximilians-Universität, 97070 Würzburg; and 2 Max-Planck-Institute of Biophysics, 60596 Frankfurt, Germany

The rat organic cation transporter (rOCT)-2 was characterized by electrical and tracer flux measurements compared with rOCT1. By applying choline gradients to voltage-clamped Xenopus oocytes expressing rOCT2, potential-dependent currents could be induced in both directions. Tracer flux measurements with seven organic cations revealed similar Michaelis-Menten constant values for both transporters, with the exception of guanidine. In parallel experiments with rOCT2 and rOCT1, inhibition of tetraethylammonium transport by 12 cations, 2 weak bases, corticosterone, and the anions para-amminohippurate, alpha -ketoglutarate, and probenecid was characterized. The IC50 values of many inhibitors were similar for both transporters, whereas others were significantly different. Mepiperphenidol and O-methylisoprenaline showed an ~70-fold lower and corticosterone a 38-fold higher affinity for rOCT2. With the use of these inhibitors together with previous information on cation transporters, experimental protocols are proposed to dissect out the individual contributions of rOCT2 and rOCT1 in intact proximal tubule preparations. Inhibition experiments at different pH levels strongly suggest that the weak base quinine passively permeates the plasma membrane at physiological pH and inhibits rOCT2 from the intracellular side.

polyspecific cation transporter; rat organic cation transporter; organic cation transporter subtypes; substrate specificity

* P. Arndt and C. Volk contributed equally to this work.




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