Gene Symbol: Slc22a1
Description: solute carrier family 22 member 1
Alias: Oct1, Orct1, Roct1, solute carrier family 22 member 1, organic cation transporter 1, solute carrier family 22 (organic cation transporter), member 1
Species: rat
Products:     Slc22a1

Top Publications

  1. Karbach U, Kricke J, Meyer Wentrup F, Gorboulev V, Volk C, Loffing Cueni D, et al. Localization of organic cation transporters OCT1 and OCT2 in rat kidney. Am J Physiol Renal Physiol. 2000;279:F679-87 pubmed
    ..In rat, the renal expression of the polyspecific cation transporters rOCT1 and rOCT2 was investigated...
  2. Zhang L, Dresser M, Chun J, Babbitt P, Giacomini K. Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A). J Biol Chem. 1997;272:16548-54 pubmed
    ..Recently, two organic cation transporters (rOCT1 and rOCT2) were cloned from rat kidney...
  3. Komazawa H, Yamaguchi H, Hidaka K, Ogura J, Kobayashi M, Iseki K. Renal uptake of substrates for organic anion transporters Oat1 and Oat3 and organic cation transporters Oct1 and Oct2 is altered in rats with adenine-induced chronic renal failure. J Pharm Sci. 2013;102:1086-94 pubmed publisher
    ..which are typical substrates for renal organic anion transporters Oat1 and Oat3 and organic cation transporters Oct1 and Oct2, respectively, were evaluated...
  4. Gong L, Goswami S, Giacomini K, Altman R, Klein T. Metformin pathways: pharmacokinetics and pharmacodynamics. Pharmacogenet Genomics. 2012;22:820-7 pubmed publisher
  5. Hu Q, Zhang X, Wang X, Jiao R, Kong L. Quercetin regulates organic ion transporter and uromodulin expression and improves renal function in hyperuricemic mice. Eur J Nutr. 2012;51:593-606 pubmed publisher
    ..These results suggest that quercetin has the uricosuric and nephroprotective actions mediated by regulating the expression levels of renal organic ion transporters and UMOD. ..
  6. Schneider R, Meusel M, Betz B, Kersten M, Moller Ehrlich K, Wanner C, et al. Nitric oxide-induced regulation of renal organic cation transport after renal ischemia-reperfusion injury. Am J Physiol Renal Physiol. 2011;301:F997-F1004 pubmed publisher
    ..the effects of iNOS-specific NO inhibition on the expression of the organic cation transporters rOct1 and rOct2 (Slc22a1 and Slc22a2, respectively) after I/R injury both in vivo and in vitro...
  7. Jin H, Hong S, Choi M, Maeng H, Kim D, Chung S, et al. Reduced antidiabetic effect of metformin and down-regulation of hepatic Oct1 in rats with ethynylestradiol-induced cholestasis. Pharm Res. 2009;26:549-59 pubmed publisher
    ..To investigate the effect of 17alpha-ethynylestradiol (EE)-induced cholestasis on the expression of organic cation transporters (Octs) in the liver and kidney, as well as the pharmacokinetics and pharmacodynamics of metformin in rats...
  8. Lips K, Luhrmann A, Tschernig T, Stoeger T, Alessandrini F, Grau V, et al. Down-regulation of the non-neuronal acetylcholine synthesis and release machinery in acute allergic airway inflammation of rat and mouse. Life Sci. 2007;80:2263-9 pubmed
    ..acetyltransferase (ChAT), the vesicular ACh transporter (VAChT), and the polyspecific organic cation transporters (OCT1-3), which are able to translocate choline and ACh across the plasma membrane...
  9. Chen Y, Currie R. Heat shock treatment suppresses angiotensin II-induced SP-1 and AP-1 and stimulates Oct-1 DNA-binding activity in heart. Inflamm Res. 2005;54:338-43 pubmed
    ..In addition, HS increased Oct-1 activity that was suppressed by Ang II infusion. These data suggest that heat shock suppresses inflammation by differentially regulating pro-inflammatory and anti-inflammatory cell signaling pathways. ..

Scientific Experts

More Information


  1. Lips K, Volk C, Schmitt B, Pfeil U, Arndt P, Miska D, et al. Polyspecific cation transporters mediate luminal release of acetylcholine from bronchial epithelium. Am J Respir Cell Mol Biol. 2005;33:79-88 pubmed
    ..Using immunohistochemistry in rats and humans, OCT1, OCT2, and OCT3 were localized to the luminal membrane of ciliated epithelial cells...
  2. Gründemann D, Gorboulev V, Gambaryan S, Veyhl M, Koepsell H. Drug excretion mediated by a new prototype of polyspecific transporter. Nature. 1994;372:549-52 pubmed
    ..Here we report the isolation of a complementary DNA from rat kidney that encodes a 556-amino-acid membrane protein, OCT1, which has the functional characteristics of organic cation uptake over the basolateral membrane of renal proximal ..
  3. Keller T, Elfeber M, Gorboulev V, Reiländer H, Koepsell H. Purification and functional reconstitution of the rat organic cation transporter OCT1. Biochemistry. 2005;44:12253-63 pubmed
    The rat organic cation transporter rOCT1 with six histidine residues added to the C-terminus was expressed in Sf9 insect cells, and expression of organic cation transport was demonstrated...
  4. Egenberger B, Gorboulev V, Keller T, Gorbunov D, Gottlieb N, Geiger D, et al. A substrate binding hinge domain is critical for transport-related structural changes of organic cation transporter 1. J Biol Chem. 2012;287:31561-73 pubmed publisher
    ..In the rat organic cation transporter (rOct1), voltage- and ligand-dependent movements of fluorescence-labeled cysteines were measured by voltage clamp ..
  5. Breidert T, Spitzenberger F, Gründemann D, Schomig E. Catecholamine transport by the organic cation transporter type 1 (OCT1). Br J Pharmacol. 1998;125:218-24 pubmed
    ..The hypothesis that OCT1 is involved the organic cation transporter type 1 which exists in rat kidney and liver-was tested. 2...
  6. Urakami Y, Okuda M, Masuda S, Saito H, Inui K. Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs. J Pharmacol Exp Ther. 1998;287:800-5 pubmed
    We have isolated a kidney-specific organic cation transporter, rat OCT2, which is distinct from rat OCT1 (Okuda M, Saito H, Urakami Y, Takano M and Inui K (1996) Biochem Biophys Res Commun 224:500-507)...
  7. Kakehi M, Koyabu N, Nakamura T, Uchiumi T, Kuwano M, Ohtani H, et al. Functional characterization of mouse cation transporter mOCT2 compared with mOCT1. Biochem Biophys Res Commun. 2002;296:644-50 pubmed
    ..1.1). Uptake of [(3)H]1-methyl-4-phenylpyridinium ([(3)H]MPP(+)) by Xenopus laevis oocytes injected with mOCT1 (Slc22a1) or mOCT2 (Slc22a2) cRNA was attenuated by an increase of extracellular K(+) concentration and under acidic ..
  8. Volk C, Gorboulev V, Kotzsch A, Müller T, Koepsell H. Five amino acids in the innermost cavity of the substrate binding cleft of organic cation transporter 1 interact with extracellular and intracellular corticosterone. Mol Pharmacol. 2009;76:275-89 pubmed publisher
    ..have shown previously that Leu447 and Gln448 in the transmembrane helix (TMH) 10 of rat organic cation transporter rOCT1 are critical for inhibition of cation uptake by corticosterone...
  9. Umehara K, Iwatsubo T, Noguchi K, Kamimura H. Functional involvement of organic cation transporter1 (OCT1/Oct1) in the hepatic uptake of organic cations in humans and rats. Xenobiotica. 2007;37:818-31 pubmed
    ..TEA), cimetidine, and metformin was examined by the use of human/rat organic cation transporter (hOCT1/rOct1)-expressing cells and human/rat hepatocytes...
  10. Grover B, Buckley D, Buckley A, Cacini W. Reduced expression of organic cation transporters rOCT1 and rOCT2 in experimental diabetes. J Pharmacol Exp Ther. 2004;308:949-56 pubmed
    ..Protein expression of the organic cation transporters rOCT1 and rOCT2 progressively decreased with increasing duration of diabetes...
  11. Keller T, Schwarz D, Bernhard F, Dötsch V, Hunte C, Gorboulev V, et al. Cell free expression and functional reconstitution of eukaryotic drug transporters. Biochemistry. 2008;47:4552-64 pubmed publisher
    ..Here, we synthesized rat organic cation transporters OCT1 and OCT2 and rat organic anion transporter OAT1 in a cell free system in the absence of detergent...
  12. Heemskerk S, Wouterse A, Russel F, Masereeuw R. Nitric oxide down-regulates the expression of organic cation transporters (OCT) 1 and 2 in rat kidney during endotoxemia. Eur J Pharmacol. 2008;584:390-7 pubmed publisher
    ..We examined the expression levels of organic cation transporter 1 (Slc22a1/Oct1) and Slc22a2/Oct2...
  13. Ulu R, Dogukan A, Tuzcu M, Gencoglu H, Ulas M, Ilhan N, et al. Regulation of renal organic anion and cation transporters by thymoquinone in cisplatin induced kidney injury. Food Chem Toxicol. 2012;50:1675-9 pubmed publisher
    ..renal injury increased protein levels of the efflux transporters MRP2 and MRP4 while expression of OAT1, OAT3, OCT1 and OCT2 was reduced...
  14. Gallegos T, Martovetsky G, Kouznetsova V, Bush K, Nigam S. Organic anion and cation SLC22 "drug" transporter (Oat1, Oat3, and Oct1) regulation during development and maturation of the kidney proximal tubule. PLoS ONE. 2012;7:e40796 pubmed publisher anion transporters Oat1 (originally identified as NKT) and Oat3 as well as the organic cation transporter Oct1. In ex vivo cultures of metanephric mesenchyme (MM; the embryonic progenitor tissue of the nephron) Oat function ..
  15. Sturm A, Gorboulev V, Gorbunov D, Keller T, Volk C, Schmitt B, et al. Identification of cysteines in rat organic cation transporters rOCT1 (C322, C451) and rOCT2 (C451) critical for transport activity and substrate affinity. Am J Physiol Renal Physiol. 2007;293:F767-79 pubmed
    ..Currents induced by 10 mM choline [I(max(choline))] in Xenopus laevis oocytes expressing rat OCT1 (rOCT1) were increased four- to ninefold after 30-s incubation with 5 mM MMTS whereas I(max(choline)) by rat OCT2 was 70% ..
  16. Yang J, Kalogerou M, Gallacher J, Sampson J, Shen M. Renal tumours in a Tsc1+/- mouse model show epigenetic suppression of organic cation transporters Slc22a1, Slc22a2 and Slc22a3, and do not respond to metformin. Eur J Cancer. 2013;49:1479-90 pubmed publisher
    ..Surprisingly, the expression of the organic cation transporters Slc22a1, Slc22a2 and Slc22a3 essential for the cellular uptake of metformin was highly suppressed in renal tumours...
  17. Hermann B, Heckert L. Silencing of Fshr occurs through a conserved, hypersensitive site in the first intron. Mol Endocrinol. 2005;19:2112-31 pubmed
    ..The findings reveal that OCT-1 binds within DHS3 to silence Fshr transcription and implicate members of the GATA family in the modulation of this activity. ..
  18. Minuesa G, Volk C, Molina Arcas M, Gorboulev V, Erkizia I, Arndt P, et al. Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3. J Pharmacol Exp Ther. 2009;329:252-61 pubmed publisher
    ..Finally, 3TC is a novel substrate for hOCTs and the inhibition of its uptake at low concentrations of ABC and AZT could have implications for the pharmacokinetics of 3TC. ..
  19. Xu L, Matsumoto A, Sasaki A, Harada H, Taniguchi A. Identification of a suppressor element in the amelogenin promoter. J Dent Res. 2010;89:246-51 pubmed publisher
    ..Mutation of the Oct-1 binding sites reversed the suppressor activity, suggesting that Oct-1 sites are essential for suppression. These results suggest that Oct-1 and intron 1 may contribute to cell-type-specific amelogenin expression. ..
  20. Kurata T, Muraki Y, Mizutani H, Iwamoto T, Okuda M. Elevated systemic elimination of cimetidine in rats with acute biliary obstruction: the role of renal organic cation transporter OCT2. Drug Metab Pharmacokinet. 2010;25:328-34 pubmed
    ..These results demonstrate that the renal tubular secretion of cimetidine was increased by acute cholestasis, and this increase was attributable to elevated expression levels of rOCT2 but not of rMATE1 in the rat. ..
  21. Wang C, Wang Y, Wang X, Zhang X, Ye J, Hu L, et al. Mulberroside a possesses potent uricosuric and nephroprotective effects in hyperuricemic mice. Planta Med. 2011;77:786-94 pubmed publisher
    ..These data suggest that mulberroside A may be a new drug candidate for the treatment of hyperuricemia with renal dysfunction. ..
  22. Keller T, Egenberger B, Gorboulev V, Bernhard F, Uzelac Z, Gorbunov D, et al. The large extracellular loop of organic cation transporter 1 influences substrate affinity and is pivotal for oligomerization. J Biol Chem. 2011;286:37874-86 pubmed publisher
    ..In the present study, evidence is provided that the large extracellular loops (EL) of rat Oct1 (rOct1) and rat Oat1 (rOat1) mediate homo- but not hetero-oligomerization...
  23. Maeda T, Goto A, Kobayashi D, Tamai I. Transport of organic cations across the blood-testis barrier. Mol Pharm. 2007;4:600-7 pubmed
    ..In addition, OCT1, OCT3, OCTN1, and OCTN2 were expressed in Sertoli cells...