Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 37, 2007 - Issue 6
389
Views
38
CrossRef citations to date
0
Altmetric
Research Article

Comparison of the kinetic characteristics of inhibitory effects exerted by biguanides and H2-blockers on human and rat organic cation transporter-mediated transport: Insight into the development of drug candidates

, , &
Pages 618-634 | Received 19 Feb 2007, Accepted 14 Apr 2007, Published online: 22 Sep 2008

References

  • Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, et al. Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. American Journal of Physiology. Renal Physiology 2001; 281: F454–468
  • Bourdet DL, Pritchard JB, Thakker DR. Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). Journal of Pharmacology and Experimental Therapeutics 2005; 315: 1288–1297
  • Cheng Y, Prusoff WH. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochemical Pharmacology 1973; 22: 3099–3108
  • Dudley AJ, Bleasby K, Brown CD. The organic cation transporter OCT2 mediates the uptake of beta-adrenoceptor antagonists across the apical membrane of renal LLC-PK(1) cell monolayers. British Journal of Pharmacology 2000; 131: 71–79
  • Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H. Cloning and characterization of two human polyspecific organic cation transporters. DNA and Cell Biology 1997; 16: 871–881
  • Gorboulev V, Volk C, Arndt P, Akhoundova A, Koepsell H. Selectivity of the polyspecific cation transporter rOCT1 is changed by mutation of aspartate 475 to glutamate. Molecular Pharmacology 1999; 56: 1254–1261
  • Gramatte T, el Desoky E, Klotz U. Site-dependent small intestinal absorption of ranitidine. European Journal of Clinical Pharmacology 1994; 46: 253–259
  • Grimson TA. Reactions to cimetidine. Lancet 1977; 1: 858
  • Grundemann D, Gorboulev V, Gambaryan S, Veyhl M, Koepsell H. Drug excretion mediated by a new prototype of polyspecific transporter. Nature 1994; 372: 549–552
  • Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E. Selective substrates for non-neuronal monoamine transporters. Molecular Pharmacology 1999; 56: 1–10
  • Grundemann D, Hahne C, Berkels R, Schomig E. Agmatine is efficiently transported by non-neuronal monoamine transporters extraneuronal monoamine transporter (EMT) and organic cation transporter 2 (OCT2). Journal of Pharmacology and Experimental Therapeutics 2003; 304: 810–817
  • Hardman JG, Molinoff PB, Ruddon RW, Gilman AG. Goodman & Gilman's. The Pharmacological Basis of Therapeutics9th. McGraw-Hill, New York 1996
  • Iwai M, Suzuki H, Ieiri I, Otsubo K, Sugiyama Y. Functional analysis of single nucleotide polymorphisms of hepatic organic anion transporter OATP1B1 (OATP-C). Pharmacogenetics 2004; 14: 749–757
  • Jonker JW, Schinkel AH. Pharmacological and physiological functions of the polyspecific organic cation transporters: OCT1, 2, and 3 (SLC22A1-3). Journal of Pharmacology and Experimental Therapeutics 2004; 308: 2–9
  • Kekuda R, Prasad PD, Wu X, Wang H, Fei YJ, Leibach FH, Ganapathy V. Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta. Journal of Biological Chemistry 1998; 273: 15971–15979
  • Kimura N, Masuda S, Tanihara Y, Ueo H, Okuda M, Katsura T, Inui K. Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1. Drug Metabolism and Pharmacokinetics 2005; 20: 379–386
  • Koepsell H, Schmitt BM, Gorboulev V. Organic cation transporters. Reviews of Physiology. Biochemistry and Pharmacology 2003; 150: 36–90
  • Lin JH. Pharmacokinetic and pharmacodynamic properties of histamine H2-receptor antagonists. Relationship between intrinsic potency and effective plasma concentrations. Clinical Pharmacokinetics 1991; 20: 218–236
  • McGuigan JE. A consideration of the adverse effects of cimetidine. Gastroenterology 1981; 80: 181–192
  • Motohashi H, Uwai Y, Hiramoto K, Okuda M, Inui K. Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A). European Journal of Pharmacology 2004; 503: 25–30
  • Nestler JE. Metformin and the polycystic ovary syndrome. Journal of Clinical Endocrinology and Metabolism 2001; 86: 1430
  • Okuda M, Saito H, Urakami Y, Takano M, Inui K. cDNA cloning and functional expression of a novel rat kidney organic cation transporter, OCT2. Biochemical and Biophysical Research Communications 1996; 224: 500–507
  • Sakata T, Anzai N, Shin HJ, Noshiro R, Hirata T, Yokoyama H, Kanai Y, Endou H. Novel single nucleotide polymorphisms of organic cation transporter 1 (SLC22A1) affecting transport functions. Biochemical and Biophysical Research Communications 2004; 313: 789–793
  • Shang T, Uihlein AV, Van Asten J, Kalyanaraman B, Hillard CJ. 1-Methyl-4-phenylpyridinium accumulates in cerebellar granule neurons via organic cation transporter 3. Journal of Neurochemistry 2003; 85: 358–367
  • Somogyi A, Stockley C, Keal J, Rolan P, Bochner F. Reduction of metformin renal tubular secretion by cimetidine in man. British Journal of Clinical Pharmacology 1987; 23: 545–551
  • Tahara H, Kusuhara H, Endou H, Koepsell H, Imaoka T, Fuse E, Sugiyama Y. A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. Journal of Pharmacology and Experimental Therapeutics 2005; 315: 337–345
  • Tucker GT, Casey C, Phillips PJ, Connor H, Ward JD, Woods HF. Metformin kinetics in healthy subjects and in patients with diabetes mellitus. British Journal of Clinical Pharmacology 1981; 12: 235–246
  • Urakami Y, Okuda M, Masuda S, Saito H, Inui KI. Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs. Journal of Pharmacology and Experimental Therapeutics 1998; 287: 800–805
  • Urakami Y, Akazawa M, Saito H, Okuda M, Inui K. cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. Journal of the American Society of Nephrology 2002; 13: 1703–1710
  • Wang DS, Jonker JW, Kato Y, Kusuhara H, Schinkel AH, Sugiyama Y. Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. Journal of Pharmacology and Experimental Therapeutics 2002; 302: 510–515
  • Wu X, Huang W, Ganapathy ME, Wang H, Kekuda R, Conway SJ, Leibach FH, Ganapathy V. Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney. American Journal of Physiology. Renal Physiology 2000; 279: F449–458
  • Yamaoka K, Tanigawara Y, Nakagawa T, Uno T. A pharmacokinetic analysis program (multi) for microcomputer. Journal of Pharmacobio-Dynamics 1981; 4: 879–885
  • Yamazaki M, Tokui T, Ishigami M, Sugiyama Y. Tissue-selective uptake of pravastatin in rats: Contribution of a specific carrier-mediated uptake system. Biopharmaceutics and Drug Disposition 1996; 17: 775–789
  • Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM. Cloning and functional expression of a human liver organic cation transporter. Molecular Pharmacology 1997; 51: 913–921

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.