organic cation transporter 1


Summary: An organic cation transporter found in kidney. It is localized to the basal lateral membrane and is likely to be involved in the renal secretion of organic cations.

Top Publications

  1. 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
    ..5. The findings demonstrate that OCTI efficiently transports catecholamines and other biogenic amines and support the hypothesis that OCT1 is responsible for hepatic and renal inactivation of circulating catecholamines. ..
  2. Moaddel R, Ravichandran S, Bighi F, Yamaguchi R, Wainer I. Pharmacophore modelling of stereoselective binding to the human organic cation transporter (hOCT1). Br J Pharmacol. 2007;151:1305-14 pubmed
    ..The pharmacophore model describes stereoselective interactions with hOCT1 at one of the binding sites on the molecule. ..
  3. Giannoudis A, Davies A, Lucas C, Harris R, Pirmohamed M, Clark R. Effective dasatinib uptake may occur without human organic cation transporter 1 (hOCT1): implications for the treatment of imatinib-resistant chronic myeloid leukemia. Blood. 2008;112:3348-54 pubmed publisher
    ..previously shown that imatinib uptake into chronic myeloid leukemia (CML) cells is dependent on human organic cation transporter 1 (hOCT1; SLC22A1), and that low hOCT1 expression is an important determinant of clinical outcome to ..
  4. Yonezawa A, Masuda S, Yokoo S, Katsura T, Inui K. Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006;319:879-86 pubmed
    ..These transporters could play predominant roles in the tissue distribution and anticancer effects and/or adverse effects of platinum agent-based chemotherapy. ..
  5. Zhang L, Dresser M, Gray A, Yost S, Terashita S, Giacomini K. Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol. 1997;51:913-21 pubmed
  6. Hirayama C, Watanabe H, Nakashima R, Nanbu T, Hamada A, Kuniyasu A, et al. Constitutive overexpression of P-glycoprotein, rather than breast cancer resistance protein or organic cation transporter 1, contributes to acquisition of imatinib-resistance in K562 cells. Pharm Res. 2008;25:827-35 pubmed
    ..Specifically, we focused on the efflux transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), and an influx transporter, organic cation transporter 1 (OCT1).
  7. Thomas J, Wang L, Clark R, Pirmohamed M. Active transport of imatinib into and out of cells: implications for drug resistance. Blood. 2004;104:3739-45 pubmed
    ..with transport inhibitors showed that verapamil, amantadine, and procainamide, inhibitors of the human organic cation transporter 1 (hOCT1), significantly decreased imatinib uptake into CEM cells, whereas the inhibition of hOCT2 or ..
  8. Chen Y, Zhang S, Sorani M, Giacomini K. Transport of paraquat by human organic cation transporters and multidrug and toxic compound extrusion family. J Pharmacol Exp Ther. 2007;322:695-700 pubmed
    ..These transporters may play an important role in the accumulation and renal excretion of PQ, and they may serve as molecular targets for the prevention and treatment of PQ-induced nephrotoxicity. ..
  9. Giannoudis A, Wang L, Jorgensen A, Xinarianos G, Davies A, Pushpakom S, et al. The hOCT1 SNPs M420del and M408V alter imatinib uptake and M420del modifies clinical outcome in imatinib-treated chronic myeloid leukemia. Blood. 2013;121:628-37 pubmed publisher
    ..These data demonstrate that the common M420del SNP can modulate the outcome of imatinib treatment. ..

More Information


  1. Gupta S, Wulf G, Henjakovic M, Koepsell H, Burckhardt G, Hagos Y. Human organic cation transporter 1 is expressed in lymphoma cells and increases susceptibility to irinotecan and paclitaxel. J Pharmacol Exp Ther. 2012;341:16-23 pubmed publisher
    ..chronic lymphocytic leukemia patients demonstrated significant expression of SLC22A1 mRNA coding for organic cation transporter 1 (OCT1)...
  2. Ciarimboli G, Struwe K, Arndt P, Gorboulev V, Koepsell H, Schlatter E, et al. Regulation of the human organic cation transporter hOCT1. J Cell Physiol. 2004;201:420-8 pubmed
    ..Regulation pathways were the same in the two expression systems. Since apparent substrate affinities depend on activity of regulatory pathways, the expression system plays a role in determining the substrate affinities. ..
  3. Gorboulev V, Ulzheimer J, Akhoundova A, Ulzheimer Teuber I, Karbach U, Quester S, et al. Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997;16:871-81 pubmed
    ..Cation transport in distal tubules is indicated for the first time. Here hOCT2 mediates the first step in cation reabsorption. hOCT1 may participate in hepatic excretion of organic cations. ..
  4. Kimura N, Masuda S, Tanihara Y, Ueo H, Okuda M, Katsura T, et al. Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1. Drug Metab Pharmacokinet. 2005;20:379-86 pubmed
    ..These findings suggest that metformin is a superior substrate for renal OCT2 rather than hepatic OCT1, and renal OCT2 plays a dominant role for metformin pharmacokinetics. ..
  5. van Montfoort J, Muller M, Groothuis G, Meijer D, Koepsell H, Meier P. Comparison of "type I" and "type II" organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001;298:110-5 pubmed
    ..type II organic cation uptake, we compared the organic cation transport properties of the rat and human organic cation transporter 1 (rOCT1; hOCT1) and of the organic anion-transporting polypeptides 2 and A (rat Oatp2; human OATP-A) in ..
  6. Moreno Navarrete J, Ortega F, Rodríguez Hermosa J, Sabater M, Pardo G, Ricart W, et al. OCT1 Expression in adipocytes could contribute to increased metformin action in obese subjects. Diabetes. 2011;60:168-76 pubmed publisher
    ..OCT1 gene expression and protein levels are detectable in adipose tissue. Increased OCT1 gene expression in adipose tissue of obese subjects might contribute to increased metformin action in these subjects. ..
  7. White D, Saunders V, Dang P, Engler J, Venables A, Zrim S, et al. Most CML patients who have a suboptimal response to imatinib have low OCT-1 activity: higher doses of imatinib may overcome the negative impact of low OCT-1 activity. Blood. 2007;110:4064-72 pubmed
    ..This pretherapy assay identifies patients at greatest risk of suboptimal response where dose intensity is critical, and those likely to respond equally well to standard dose imatinib. ..
  8. Kerb R, Brinkmann U, Chatskaia N, Gorbunov D, Gorboulev V, Mornhinweg E, et al. Identification of genetic variations of the human organic cation transporter hOCT1 and their functional consequences. Pharmacogenetics. 2002;12:591-5 pubmed
  9. Iwai M, Minematsu T, Narikawa S, Usui T, Kamimura H. Involvement of human organic cation transporter 1 in the hepatic uptake of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazolium bromide (YM155 monobromide), a novel, small molecule survivin suppressant. Drug Metab Dispos. 2009;37:1856-63 pubmed publisher
  10. 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
    ..These results suggested that both OCT1 and OCT2 are basolateral-type organic cation transporters with broad substrate specificities, mediating tubular secretion of cationic drugs. ..
  11. Wang D, Jonker J, Kato Y, Kusuhara H, Schinkel A, Sugiyama Y. Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. J Pharmacol Exp Ther. 2002;302:510-5 pubmed
    ..The purpose of the present study was to investigate the role of organic cation transporter 1 (Oct1) in the disposition of metformin...
  12. Ahlin G, Karlsson J, Pedersen J, Gustavsson L, Larsson R, Matsson P, et al. Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. J Med Chem. 2008;51:5932-42 pubmed publisher
    ..The data were used to generate OPLS-DA models for OCT1 inhibitors; the final model correctly predicted 82% of the inhibitors and 88% of the noninhibitors of the test set. ..
  13. Li S, Chen Y, Zhang S, More S, Huang X, Giacomini K. Role of organic cation transporter 1, OCT1 in the pharmacokinetics and toxicity of cis-diammine(pyridine)chloroplatinum(II) and oxaliplatin in mice. Pharm Res. 2011;28:610-25 pubmed publisher
    The goal of this study was to test the hypothesis that by controlling intracellular uptake, organic cation transporter 1, Oct1 is a key determinant of the disposition and toxicity of cis-diammine(pyridine)chloroplatinum(II)(CDPCP) and ..
  14. Ciarimboli G, Koepsell H, Iordanova M, Gorboulev V, Dürner B, Lang D, et al. Individual PKC-phosphorylation sites in organic cation transporter 1 determine substrate selectivity and transport regulation. J Am Soc Nephrol. 2005;16:1562-70 pubmed
    ..The different effects on the EC(50) values by the different mutations suggest that the large intracellular loop participates in building the substrate binding pocket of rOCT1 or specifically modulates its structure. ..
  15. Ishiguro N, Saito A, Yokoyama K, Morikawa M, Igarashi T, Tamai I. Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney. Drug Metab Dispos. 2005;33:495-9 pubmed
    ..0 microM and 163.7, 10.7, and 47.7 microM, respectively. These results demonstrate that both rOCT1 and rOCT2 are involved in the renal uptake of pramipexole across the basolateral membrane of the proximal tubular epithelial cells. ..
  16. Lautem A, Heise M, Gräsel A, Hoppe Lotichius M, Weiler N, Foltys D, et al. Downregulation of organic cation transporter 1 (SLC22A1) is associated with tumor progression and reduced patient survival in human cholangiocellular carcinoma. Int J Oncol. 2013;42:1297-304 pubmed publisher
    ..In conclusion, the downregulation of OCT1 is associated with tumor progression and worse overall patient survival rates. ..
  17. Jonker J, Wagenaar E, Van Eijl S, Schinkel A. Deficiency in the organic cation transporters 1 and 2 (Oct1/Oct2 [Slc22a1/Slc22a2]) in mice abolishes renal secretion of organic cations. Mol Cell Biol. 2003;23:7902-8 pubmed
    ..This study shows that Oct1 and Oct2 together are essential for renal secretion of (small) organic cations. A deficiency in these proteins may thus result in increased drug sensitivity and toxicity. ..
  18. Bednarczyk D, Ekins S, Wikel J, Wright S. Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1. Mol Pharmacol. 2003;63:489-98 pubmed
    ..These results indicate how a combination of computational and in vitro approaches may yield insight into the binding affinity of transporters and may be applicable to predicting these properties for new therapeutics. ..
  19. Jonker J, Schinkel A. Pharmacological and physiological functions of the polyspecific organic cation transporters: OCT1, 2, and 3 (SLC22A1-3). J Pharmacol Exp Ther. 2004;308:2-9 pubmed
  20. Chen L, Takizawa M, Chen E, Schlessinger A, Segenthelar J, Choi J, et al. Genetic polymorphisms in organic cation transporter 1 (OCT1) in Chinese and Japanese populations exhibit altered function. J Pharmacol Exp Ther. 2010;335:42-50 pubmed publisher
    b>Organic cation transporter 1 (OCT1; SLC22A1) seems to play a role in the efficacy and disposition of the widely used antidiabetic drug metformin. Genetic variants in OCT1 have been identified largely in European populations...
  21. Ming X, Ju W, Wu H, Tidwell R, Hall J, Thakker D. Transport of dicationic drugs pentamidine and furamidine by human organic cation transporters. Drug Metab Dispos. 2009;37:424-30 pubmed publisher
    ..These transporters may play important roles in the disposition of aromatic diamidines in humans, as well as resultant drug-drug interactions and toxicity involving diamidine drugs. ..
  22. Schlatter E, Mönnich V, Cetinkaya I, Mehrens T, Ciarimboli G, Hirsch J, et al. The organic cation transporters rOCT1 and hOCT2 are inhibited by cGMP. J Membr Biol. 2002;189:237-44 pubmed
    ..The data suggest that the inhibition mediated by cGMP observed in HEK293 cells occurs most likely via a mammalian cGMP-binding protein that interacts with OCT1-2 transporters. ..
  23. Lovejoy K, Todd R, Zhang S, McCormick M, D Aquino J, Reardon J, et al. cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospects. Proc Natl Acad Sci U S A. 2008;105:8902-7 pubmed publisher
    ..These exceptional characteristics indicate that cDPCP and related complexes merit consideration as therapeutic options for treating colorectal and other cancers bearing appropriate cation transporters. ..
  24. Becker M, Visser L, van Schaik R, Hofman A, Uitterlinden A, Stricker B. OCT1 polymorphism is associated with response and survival time in anti-Parkinsonian drug users. Neurogenetics. 2011;12:79-82 pubmed publisher
    Substrates for the Organic Cation Transporter 1, encoded by the SLC22A1 gene, are metformin, amantadine, pramipexole, and, possibly, levodopa...
  25. Sebastiano V, Dalvai M, Gentile L, Schubart K, Sutter J, Wu G, et al. Oct1 regulates trophoblast development during early mouse embryogenesis. Development. 2010;137:3551-60 pubmed publisher
    ..Our data also suggest that Oct1 is required in the embryo proper from late gastrulation stages onwards. ..
  26. Clark R, Davies A, Pirmohamed M, Giannoudis A. Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008;49:639-42 pubmed publisher
    ..By contrast, the influx transporter, human organic cation transporter 1 (hOCT1) (also known as SLC22A1), transports imatinib into cells...
  27. Shakya A, Kang J, Chumley J, Williams M, Tantin D. Oct1 is a switchable, bipotential stabilizer of repressed and inducible transcriptional states. J Biol Chem. 2011;286:450-9 pubmed publisher
    ..We propose that, rather than acting as a primary trigger of gene activation or repression, Oct1 is a switchable stabilizer of repressed and inducible states. ..
  28. Goralski K, Lou G, Prowse M, Gorboulev V, Volk C, Koepsell H, et al. The cation transporters rOCT1 and rOCT2 interact with bicarbonate but play only a minor role for amantadine uptake into rat renal proximal tubules. J Pharmacol Exp Ther. 2002;303:959-68 pubmed
    ..TEA uptake by the basolateral membrane may be mediated mainly by rOCT1 and rOCT2, but these transporters may be in a different functional or regulatory state when expressed in cells or oocytes compared with expression in vivo. ..
  29. Shikata E, Yamamoto R, Takane H, Shigemasa C, Ikeda T, Otsubo K, et al. Human organic cation transporter (OCT1 and OCT2) gene polymorphisms and therapeutic effects of metformin. J Hum Genet. 2007;52:117-22 pubmed
    ..In this study it is suggested that OCT1 and OCT2 gene polymorphisms have little contribution to the clinical efficacy of metformin. ..
  30. Sala Rabanal M, Li D, Dake G, Kurata H, Inyushin M, Skatchkov S, et al. Polyamine transport by the polyspecific organic cation transporters OCT1, OCT2, and OCT3. Mol Pharm. 2013;10:1450-8 pubmed publisher
    ..The identification of OCTs as polyamine transport systems may contribute to further understanding of the mechanisms involved in polyamine homeostasis and aid in the design of polyamine-like OCT-targeted drugs. ..
  31. Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H. Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002;301:293-8 pubmed
  32. Martel F, Gründemann D, Calhau C, Schomig E. Apical uptake of organic cations by human intestinal Caco-2 cells: putative involvement of ASF transporters. Naunyn Schmiedebergs Arch Pharmacol. 2001;363:40-9 pubmed
    ..Reverse transcriptase-polymerase chain reaction indicates that mRNA of hEMT and of the human organic cation transporter 1 (hOCT1) are present in Caco-2 cells...
  33. Shu Y, Sheardown S, Brown C, Owen R, Zhang S, Castro R, et al. Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action. J Clin Invest. 2007;117:1422-31 pubmed
    Metformin is among the most widely prescribed drugs for the treatment of type 2 diabetes. Organic cation transporter 1 (OCT1) plays a role in the hepatic uptake of metformin, but its role in the therapeutic effects of the drug, which ..
  34. Tarasova L, Kalnina I, Geldnere K, Bumbure A, Ritenberga R, Nikitina Zake L, et al. Association of genetic variation in the organic cation transporters OCT1, OCT2 and multidrug and toxin extrusion 1 transporter protein genes with the gastrointestinal side effects and lower BMI in metformin-treated type 2 diabetes patients. Pharmacogenet Genomics. 2012;22:659-66 pubmed publisher
    ..So far, the number of polymorphisms in SLC22A1, SLC22A2, and SLC47A1 genes coding for organic cation transporter 1 (OCT1), OCT2, and multidrug and toxin extrusion transporter 1 (MATE1) metformin transporters have been ..
  35. Yamakawa Y, Hamada A, Nakashima R, Yuki M, Hirayama C, Kawaguchi T, et al. Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011;33:244-50 pubmed publisher
  36. Wessler I, Roth E, Deutsch C, Brockerhoff P, Bittinger F, Kirkpatrick C, et al. Release of non-neuronal acetylcholine from the isolated human placenta is mediated by organic cation transporters. Br J Pharmacol. 2001;134:951-6 pubmed
    ..7. It is concluded that the release of non-neuronal acetylcholine from the human placenta is mediated via organic cation transporters of the OCT1 and OCT3 subtype. ..
  37. Zhong J, Meng F, Xu D, Zhou H, Dai M. Correlation between imatinib trough concentration and efficacy in Chinese chronic myelocytic leukemia patients. Acta Haematol. 2012;127:221-7 pubmed publisher
    ..We aimed to determine plasma imatinib concentration, intracellular imatinib concentration, human organic cation transporter 1 (hOCT1) and adenosine triphosphate-binding cassette subfamily B member 1 (ABCB1) mRNA expression in ..
  38. Dickens D, Owen A, Alfirevic A, Giannoudis A, Davies A, Weksler B, et al. Lamotrigine is a substrate for OCT1 in brain endothelial cells. Biochem Pharmacol. 2012;83:805-14 pubmed publisher
    ..Furthermore, use of a panel of transporter inhibitors indicated that this active uptake was mediated by organic cation transporter 1 (OCT1). OCT1 mRNA and protein were shown to be expressed in hCMEC/D3 cells...
  39. Schweifer N, Barlow D. The Lx1 gene maps to mouse chromosome 17 and codes for a protein that is homologous to glucose and polyspecific transmembrane transporters. Mamm Genome. 1996;7:735-40 pubmed
    ..Chr 6q has been previously associated with transient neonatal diabetes mellitus and breast cancer. ..
  40. Nardinelli L, Sanabani S, Didone A, Ferreira P, Serpa M, Novaes M, et al. Pretherapeutic expression of the hOCT1 gene predicts a complete molecular response to imatinib mesylate in chronic-phase chronic myeloid leukemia. Acta Haematol. 2012;127:228-34 pubmed publisher
    In this retrospective study we evaluated the pretherapeutic mRNA expression of the hOCT1 (human organic cation transporter 1) gene in patients with chronic-phase (CP) chronic myeloid leukemia (CML) who varied in terms of their response to ..
  41. Iwai M, Minematsu T, Li Q, Iwatsubo T, Usui T. Utility of P-glycoprotein and organic cation transporter 1 double-transfected LLC-PK1 cells for studying the interaction of YM155 monobromide, novel small-molecule survivin suppressant, with P-glycoprotein. Drug Metab Dispos. 2011;39:2314-20 pubmed publisher
    ..Transcellular assays lacking basal uptake transporters may be inaccurate in the assessment of hydrophilic compounds that have poor membrane permeability by passive diffusion. ..
  42. Gambineri A, Tomassoni F, Gasparini D, Di Rocco A, Mantovani V, Pagotto U, et al. Organic cation transporter 1 polymorphisms predict the metabolic response to metformin in women with the polycystic ovary syndrome. J Clin Endocrinol Metab. 2010;95:E204-8 pubmed publisher
    ..b>Organic cation transporter 1 (OCT1) plays a trigger role in the hepatic uptake of metformin...
  43. Tzvetkov M, Saadatmand A, Lotsch J, Tegeder I, Stingl J, Brockmoller J. Genetically polymorphic OCT1: another piece in the puzzle of the variable pharmacokinetics and pharmacodynamics of the opioidergic drug tramadol. Clin Pharmacol Ther. 2011;90:143-50 pubmed publisher
    ..005, n = 24). In conclusion, polymorphisms in OCT1 influence the pharmacokinetics of O-desmethyltramadol, presumably by affecting its uptake into liver cells, and thus may modulate the efficacy of tramadol treatment...
  44. Mulgaonkar A, Venitz J, Gründemann D, Sweet D. Human organic cation transporters 1 (SLC22A1), 2 (SLC22A2), and 3 (SLC22A3) as disposition pathways for fluoroquinolone antimicrobials. Antimicrob Agents Chemother. 2013;57:2705-11 pubmed publisher
    ..However, hOCT1 in the sinusoidal membrane of hepatocytes, and potentially the basolateral membrane of proximal tubule cells, is likely to play a role in the disposition of these antimicrobial agents. ..
  45. Koepsell H. The SLC22 family with transporters of organic cations, anions and zwitterions. Mol Aspects Med. 2013;34:413-35 pubmed publisher
    ..Drug-drug interactions at individual transporters may change pharmacokinetics and toxicities of drugs. ..
  46. Kimura N, Masuda S, Katsura T, Inui K. Transport of guanidine compounds by human organic cation transporters, hOCT1 and hOCT2. Biochem Pharmacol. 2009;77:1429-36 pubmed publisher
    ..49+/-0.14mM. These results indicated that the specificity of hOCT1 and hOCT2 was not determined simply by guanidino group. Among guanidine compounds, aminoguanidine was identified as a new superior substrate for hOCT2. ..
  47. Yang M, McLean A, Le Couteur D. Cell membrane transport of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in the liver and systemic bioavailability. Biochem Biophys Res Commun. 2001;289:130-6 pubmed
    ..Only a small proportion of MPTP is taken up into hepatocytes by transporters; however, modulation of these transport mechanisms will influence systemic bioavailability. ..
  48. Hayer Zillgen M, Bruss M, Bonisch H. Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002;136:829-36 pubmed
  49. Gründemann D, Hahne C, Berkels R, Schömig E. Agmatine is efficiently transported by non-neuronal monoamine transporters extraneuronal monoamine transporter (EMT) and organic cation transporter 2 (OCT2). J Pharmacol Exp Ther. 2003;304:810-7 pubmed
    ..Thus, only the singly charged species of agmatine is accepted as substrate. In conclusion, both EMT and OCT2 must be considered for the control of agmatine levels in rat and human. ..
  50. Shu Y, Leabman M, Feng B, Mangravite L, Huang C, Stryke D, et al. Evolutionary conservation predicts function of variants of the human organic cation transporter, OCT1. Proc Natl Acad Sci U S A. 2003;100:5902-7 pubmed
  51. Hayer M, Bonisch H, Bruss M. Molecular cloning, functional characterization and genomic organization of four alternatively spliced isoforms of the human organic cation transporter 1 (hOCT1/SLC22A1). Ann Hum Genet. 1999;63:473-82 pubmed
    ..When stably expressed in human embryonic kidney (HEK293) cells, only the full length hOCT1 cDNA mediated decynium-22 (D22)-sensitive uptake of tritiated 1-methyl-4-phenylpyridinium ([3H]-MPP+). ..
  52. Moaddel R, Patel S, Jozwiak K, Yamaguchi R, Ho P, Wainer I. Enantioselective binding to the human organic cation transporter-1 (hOCT1) determined using an immobilized hOCT1 liquid chromatographic stationary phase. Chirality. 2005;17:501-6 pubmed
    ..75]. The chromatographically determined K(d) values were used to construct an initial pharmacophore which contains a hydrogen bond donating site that appears to be responsible for the observed enantioselectivity. ..
  53. Bourdet D, Pritchard J, Thakker D. Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). J Pharmacol Exp Ther. 2005;315:1288-97 pubmed
    ..Famotidine seems to be one of the most potent inhibitors of hOCT3 yet identified. ..
  54. Saborowski M, Kullak Ublick G, Eloranta J. The human organic cation transporter-1 gene is transactivated by hepatocyte nuclear factor-4alpha. J Pharmacol Exp Ther. 2006;317:778-85 pubmed
    ..In conclusion, the hOCT1 gene, encoding an important drug transporter in the human liver, is activated by HNF-4alpha and suppressed by bile acids via SHP. ..
  55. 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
  56. Nies A, Herrmann E, Brom M, Keppler D. Vectorial transport of the plant alkaloid berberine by double-transfected cells expressing the human organic cation transporter 1 (OCT1, SLC22A1) and the efflux pump MDR1 P-glycoprotein (ABCB1). Naunyn Schmiedebergs Arch Pharmacol. 2008;376:449-61 pubmed
    ..Madin-Darby canine kidney strain II (MDCKII) cell line permanently expressing the human organic cation transporter 1 (OCT1, SLC22A1) in the basolateral membrane and MDR1 P-glycoprotein (MDR1 P-gp, ABCB1), an adenosine ..
  57. Hu S, Franke R, Filipski K, Hu C, Orwick S, De Bruijn E, et al. Interaction of imatinib with human organic ion carriers. Clin Cancer Res. 2008;14:3141-8 pubmed publisher
    The activity of imatinib in leukemia has recently been linked with expression of the organic cation transporter 1 (OCT1) gene SLC22A1...
  58. Jung N, Lehmann C, Rubbert A, Knispel M, Hartmann P, van Lunzen J, et al. Relevance of the organic cation transporters 1 and 2 for antiretroviral drug therapy in human immunodeficiency virus infection. Drug Metab Dispos. 2008;36:1616-23 pubmed publisher
    ..These data suggest that drug interactions about the OCTs may be relevant for the ARV therapy, in particular by influencing drug accession to infected tissues and hepatic or renal elimination. ..
  59. White D, Dang P, Engler J, Frede A, Zrim S, Osborn M, et al. Functional activity of the OCT-1 protein is predictive of long-term outcome in patients with chronic-phase chronic myeloid leukemia treated with imatinib. J Clin Oncol. 2010;28:2761-7 pubmed publisher
    ..Early dose-intensity may reduce the negative prognostic impact of low OA. We propose that OA could be used to individualize dosage strategies for patients with CML to maximize molecular response and optimize long-term outcome. ..
  60. Meyer Wentrup F, Karbach U, Gorboulev V, Arndt P, Koepsell H. Membrane localization of the electrogenic cation transporter rOCT1 in rat liver. Biochem Biophys Res Commun. 1998;248:673-8 pubmed
    ..Translational regulation is suggested since the message of rOCT1 was distributed throughout the liver lobuli, whereas rOCT1 protein was observed only in hepatocytes surrounding the central veins. ..
  61. Green R, Lo K, Sterritt C, Beier D. Cloning and functional expression of a mouse liver organic cation transporter. Hepatology. 1999;29:1556-62 pubmed
    ..mOct1/Slc22a1 encodes for a hepatic and renal organic cation transporter which may be important for the uptake and secretion of cationic drugs and endobiotics. ..
  62. 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
    ..As OCT1 translocates hydrophobic and hydrophilic organic cations of different structures, it is considered to be a new prototype of polyspecific transporters that are important for drug elimination. ..
  63. O Brien V, Bokelmann K, Ramirez J, Jobst K, Ratain M, Brockmoller J, et al. Hepatocyte nuclear factor 1 regulates the expression of the organic cation transporter 1 via binding to an evolutionary conserved region in intron 1 of the OCT1 gene. J Pharmacol Exp Ther. 2013;347:181-92 pubmed publisher
    The organic cation transporter 1 (OCT1), also known as solute carrier family 22 member 1, is strongly and specifically expressed in the human liver...
  64. Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K. Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001;18:1528-34 pubmed
  65. Horvath G, Sutto Z, Torbati A, Conner G, Salathe M, Wanner A. Norepinephrine transport by the extraneuronal monoamine transporter in human bronchial arterial smooth muscle cells. Am J Physiol Lung Cell Mol Physiol. 2003;285:L829-37 pubmed
    ..RT-PCR demonstrated mRNA expression of the extraneuronal monoamine transporter (EMT) and organic cation transporter 1 (OCT-1)...
  66. Itoda M, Saito Y, Maekawa K, Hichiya H, Komamura K, Kamakura S, et al. Seven novel single nucleotide polymorphisms in the human SLC22A1 gene encoding organic cation transporter 1 (OCT1). Drug Metab Pharmacokinet. 2004;19:308-12 pubmed
    ..genetic variations, including seven novel ones, were found in the human SLC22A1 gene, which encodes organic cation transporter 1, from 116 Japanese individuals...
  67. Maffioli M, Camos M, Gaya A, Hernández Boluda J, Alvarez Larran A, Domingo A, et al. Correlation between genetic polymorphisms of the hOCT1 and MDR1 genes and the response to imatinib in patients newly diagnosed with chronic-phase chronic myeloid leukemia. Leuk Res. 2011;35:1014-9 pubmed publisher
    ..Beside, the MDR1 haplotype 1236T-2677G-3435C was more frequently found in patients primarily resistant to imatinib. ..
  68. Tzvetkov M, Saadatmand A, Bokelmann K, Meineke I, Kaiser R, Brockmoller J. Effects of OCT1 polymorphisms on the cellular uptake, plasma concentrations and efficacy of the 5-HT(3) antagonists tropisetron and ondansetron. Pharmacogenomics J. 2012;12:22-9 pubmed publisher
    ..We investigated whether the hepatic organic cation transporter 1 (OCT1; SLC22A1) mediates cellular uptake and whether common OCT1 loss-of-function polymorphisms affect ..
  69. Hiwase D, Saunders V, Hewett D, Frede A, Zrim S, Dang P, et al. Dasatinib cellular uptake and efflux in chronic myeloid leukemia cells: therapeutic implications. Clin Cancer Res. 2008;14:3881-8 pubmed publisher
    ..The relevance of OCT-1 activity and efflux pumps in determining intracellular uptake and retention (IUR) of dasatinib was assessed...