Electrogenic properties and substrate specificity of the polyspecific rat cation transporter rOCT1.
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Busch AE, Quester S, Ulzheimer JC, Waldegger S, Gorboulev V, Arndt P, Lang F, Koepsell H
Electrogenic properties and substrate specificity of the polyspecific rat cation transporter rOCT1.
J Biol Chem. 1996 Dec 20;271(51):32599-604.
- PubMed ID
- 8955087 [ View in PubMed]
- Abstract
The previously cloned rat cation transporter rOCT1 detected in renal proximal tubules and hepatocytes (Grundemann, D., Gorboulev, V., Gambaryan, S., Veyhl, M., and Koepsell, H. (1994) Nature 372, 549-552) was expressed in Xenopus oocytes, and transport properties were analyzed using tracer uptake studies and electrophysiological measurements. rOCT1 induced highly active transport of a variety of cations, including the classical substrates for cation transport, such as N-1-methylnicotinamide, 1-methyl-4-phenylpyridinium (MPP), and tetraethylammonium (TEA), but also the physiologically important choline. In oocytes rOCT1 also mediated efflux of MPP, which could be trans-stimulated by MPP and TEA. Cation transport via rOCT1 was electrogenic. In voltage-clamped oocytes, transport of TEA and choline via rOCT1 produced inwardly directed currents, which were independent of extracellular ion composition or pH. The choline- and TEA-induced currents were voltage-dependent at nonsaturating concentrations, and the apparent affinity of these cations was decreased at depolarized voltages. Other substrates transported by rOCT1 were the polyamines spermine and spermidine. Interestingly, the previously described potent inhibitors of rOCT1, cyanine 863, quinine, and D-tubocurarine were substrates themselves. The data indicate that rOCT1 is an effective transport system that is responsible for electrogenic uptake of a wide variety of organic cations into epithelial cells of renal proximal tubules and hepatocytes.
DrugBank Data that Cites this Article
- Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Choline Solute carrier family 22 member 1 Protein Humans UnknownSubstrateInhibitorDetails Choline salicylate Solute carrier family 22 member 1 Protein Humans UnknownSubstrateInhibitorDetails Quinidine Solute carrier family 22 member 1 Protein Humans UnknownInhibitorDetails Quinine Solute carrier family 22 member 1 Protein Humans UnknownSubstrateInhibitorDetails Spermidine Solute carrier family 22 member 1 Protein Humans UnknownSubstrateDetails Spermine Solute carrier family 22 member 1 Protein Humans UnknownSubstrateDetails Tubocurarine Solute carrier family 22 member 1 Protein Humans UnknownSubstrateDetails