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Gene Review

Slc22a2  -  solute carrier family 22 (organic cation...

Rattus norvegicus

Synonyms: OCT2, OCT2r, Oct2, Organic cation transporter 2, Solute carrier family 22 member 2, ...
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Disease relevance of Slc22a2

  • Association between tubular toxicity of cisplatin and expression of organic cation transporter rOCT2 (Slc22a2) in the rat [1].
  • Adenovirus also produced a dose-dependent increase in immunoreactive OCT-2 levels concomitant with increased cellular OCT-2 steady-state mRNA [2].
  • Furthermore, our RT-PCR analyses reveal the presence of mRNA for novel organic cation transporters 1 and 2 (OCTN1 and OCTN2), but not for OCT1 or OCT2 in the ganglion [3].
  • Restored expression and activity of organic ion transporters rOAT1, rOAT3 and rOCT2 after hyperuricemia in the rat kidney [4].

High impact information on Slc22a2


Chemical compound and disease context of Slc22a2

  • The plasma testosterone concentration, which is a dominant factor in the regulation of rOCT2, was gradually restored during the recovery from hyperuricemia, but the correlation between the plasma testosterone level and rOCT2 protein expression in the kidney was not significant [4].
  • Basolateral uptake of p-aminohippurate (PAH) and tetraethylammonium (TEA), and both protein and mRNA levels of rOAT1, rOAT3 and rOCT2 in the kidney gradually improved during 14 days of recovery from hyperuricemia [4].

Biological context of Slc22a2

  • In addition, our data, when compared with previous studies, suggest that OCT2 corresponds to the organic cation/H+ antiport mechanism in renal brush-border membrane vesicles, and that EMT corresponds to the guanidine/H+ antiport mechanism in membrane vesicles from placenta and intestine [8].
  • The rat OCT2 cDNA (2,205 bp) had an open reading frame encoding for a 593-amino acid protein (calculated molecular mass of 66 kDa) which shows 67% identity with the rat OCT1 [9].
  • The data suggest that the substrate binding site of rOCT2 is like a pocket containing overlapping binding domains for ligands [10].
  • For example, the IC50 values for corticosterone inhibition of cation uptake by transporters rOCT1 and rOCT2 are approximately 150 and approximately 4 microM, respectively [11].
  • These results suggested that both OCT1 and OCT2 are basolateral-type organic cation transporters with broad substrate specificities, mediating tubular secretion of cationic drugs [12].

Anatomical context of Slc22a2

  • PCR products for the choline transporters, OCT-1 and OCT-2, were detected, but only OCT-2 protein was robustly expressed within MLE and primary alveolar epithelial cells [2].
  • Northern hybridization and reverse transcription-PCR analyses revealed that the rat OCT2 mRNA transcript was expressed predominantly in the kidney, at higher level in the medulla than in the cortex, but this transcript was not detected in the brain, heart, lung, liver, small intestine or spleen [9].
  • An OCT2-specific probe produced signals in the zona glomerulosa and outer zona fasciculata [13].
  • RT-PCR demonstrated that astrocytes expressed low levels of OCT1, OCT2 and OCT3 mRNA, but the functional characteristics of choline uptake are very different from the known properties of these OCTs [14].
  • To further evaluate the nature of the pH effect and assess the properties of rOCT2 in a renal epithelium, rOCT2 was introduced into MDCK cells [15].

Associations of Slc22a2 with chemical compounds


Analytical, diagnostic and therapeutic context of Slc22a2


  1. Association between tubular toxicity of cisplatin and expression of organic cation transporter rOCT2 (Slc22a2) in the rat. Yonezawa, A., Masuda, S., Nishihara, K., Yano, I., Katsura, T., Inui, K. Biochem. Pharmacol. (2005) [Pubmed]
  2. Adenovirus stimulates choline efflux by increasing expression of organic cation transporter-2. Miakotina, O.L., Agassandian, M., Shi, L., Look, D.C., Mallampalli, R.K. Am. J. Physiol. Lung Cell Mol. Physiol. (2005) [Pubmed]
  3. Organic cation transporter mRNA and function in the rat superior cervical ganglion. Kristufek, D., Rudorfer, W., Pifl, C., Huck, S. J. Physiol. (Lond.) (2002) [Pubmed]
  4. Restored expression and activity of organic ion transporters rOAT1, rOAT3 and rOCT2 after hyperuricemia in the rat kidney. Habu, Y., Yano, I., Okuda, M., Fukatsu, A., Inui, K. Biochem. Pharmacol. (2005) [Pubmed]
  5. Alkali cation binding and permeation in the rat organic cation transporter rOCT2. Schmitt, B.M., Koepsell, H. J. Biol. Chem. (2005) [Pubmed]
  6. Ventricular choline transport: a role for organic cation transporter 2 expressed in choroid plexus. Sweet, D.H., Miller, D.S., Pritchard, J.B. J. Biol. Chem. (2001) [Pubmed]
  7. Transport of monoamine transmitters by the organic cation transporter type 2, OCT2. Gründemann, D., Köster, S., Kiefer, N., Breidert, T., Engelhardt, M., Spitzenberger, F., Obermüller, N., Schömig, E. J. Biol. Chem. (1998) [Pubmed]
  8. Selective substrates for non-neuronal monoamine transporters. Gründemann, D., Liebich, G., Kiefer, N., Köster, S., Schömig, E. Mol. Pharmacol. (1999) [Pubmed]
  9. cDNA cloning and functional expression of a novel rat kidney organic cation transporter, OCT2. Okuda, M., Saito, H., Urakami, Y., Takano, M., Inui, K. Biochem. Biophys. Res. Commun. (1996) [Pubmed]
  10. Different affinities of inhibitors to the outwardly and inwardly directed substrate binding site of organic cation transporter 2. Volk, C., Gorboulev, V., Budiman, T., Nagel, G., Koepsell, H. Mol. Pharmacol. (2003) [Pubmed]
  11. Subtype-specific affinity for corticosterone of rat organic cation transporters rOCT1 and rOCT2 depends on three amino acids within the substrate binding region. Gorboulev, V., Shatskaya, N., Volk, C., Koepsell, H. Mol. Pharmacol. (2005) [Pubmed]
  12. Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs. Urakami, Y., Okuda, M., Masuda, S., Saito, H., Inui, K.I. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  13. Molecular evidence of organic ion transporters in the rat adrenal cortex with adrenocorticotropin-regulated zonal expression. Béery, E., Middel, P., Bahn, A., Willenberg, H.S., Hagos, Y., Koepsell, H., Bornstein, S.R., Müller, G.A., Burckhardt, G., Steffgen, J. Endocrinology (2003) [Pubmed]
  14. Molecular and functional characterization of an Na+-independent choline transporter in rat astrocytes. Inazu, M., Takeda, H., Matsumiya, T. J. Neurochem. (2005) [Pubmed]
  15. rOCT2 is a basolateral potential-driven carrier, not an organic cation/proton exchanger. Sweet, D.H., Pritchard, J.B. Am. J. Physiol. (1999) [Pubmed]
  16. Mutation of amino acid 475 of rat organic cation transporter 2 (rOCT2) impairs organic cation transport. Bahn, A., Hagos, Y., Rudolph, T., Burckhardt, G. Biochimie (2004) [Pubmed]
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