Authors: Muller, Ingo; Hagos, Yohannes; Burckhardt, Gerhard; Burckhardt, Birgitta C.

Source: Letters in Drug Design & Discovery, Volume 2, Number 7, November 2005 , pp. 567-570(4)

Publisher: Bentham Science Publishers

Abstract:

Renal elimination of drugs bound to plasma proteins is mediated mainly by tubular secretion. Furosemide, a frequently used diuretic, is tightly bound to plasma proteins and is believed to be secreted. It contains a carboxyl group and a sulfamoyl moiety and may therefore be a substrate for the sodium-dependent dicarboxylate cotransporter from human kidney (hNaDC-3). Furosemide, besides inhibiting [14C]succinate uptake, reduced succinate-associated currents in a dose-dependent manner with an IC50 of 2.2 mM. Furosemide showed sodium-dependent inward currents as evidence for its translocation by hNaDC-3. The concentrations necessary to affect hNaDC-3, however, are far higher than the therapeutically relevant plasma concentrations of furosemide. This implies that dicarboxylate uptake necessary for drug excretion via organic anion/dicarboxylate exchange will not be altered by therapeutical doses of furosemide.

Keywords: Furosemide; human kidney; organic anion transporters 1 and 3; sodium-dependent dicarboxylate transporter

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157018005774479087

Affiliations: 1: Zentrum Physiologie und Pathophysiologie, Abt. Vegetative Physiologie und Pathophysiologie, Georg August Universitat Gottingen, Humboldtallee 23, 37073 Gottingen, Germany

Publication date: 2005-11-01

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• Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

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