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Xenobiotica
the fate of foreign compounds in biological systems
Volume 37, 2007 - Issue 6
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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

K.-I. Umehara Drug Metabolism Research Laboratories, Drug Discovery Research, Astellas Pharma Inc., Tokyo, Japan
,
T. Iwatsubo Drug Metabolism Research Laboratories, Drug Discovery Research, Astellas Pharma Inc., Tokyo, Japan
,
K. Noguchi Drug Metabolism Research Laboratories, Drug Discovery Research, Astellas Pharma Inc., Tokyo, Japan
&
H. Kamimura Drug Metabolism Research Laboratories, Drug Discovery Research, Astellas Pharma Inc., Tokyo, Japan
Pages 618-634 | Received 19 Feb 2007, Accepted 14 Apr 2007, Published online: 22 Sep 2008

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Naotoshi Yamamura, Tomoki Imaoka, Misa Hoshi, Makiko Yamada & Ken-ichi Itokawa. (2023) Renal tubular transporter-mediated interactions between mirogabalin and cimetidine in rats. Xenobiotica 53:2, pages 114-122.
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Jürgen Kindla, Martin F Fromm & Jörg König. (2009) In vitro evidence for the role of OATP and OCT uptake transporters in drug–drug interactions. Expert Opinion on Drug Metabolism & Toxicology 5:5, pages 489-500.
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K.-I. Umehara, K. Seya, T. Iwatsubo, K. Noguchi, T. Usui & H. Kamimura. (2008) Tissue distribution of YM758, a novel If channel inhibitor, in pregnant and lactating rats. Xenobiotica 38:10, pages 1274-1288.
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K.-I. Umehara, T. Iwatsubo, K. Noguchi, T. Usui & H. Kamimura. (2008) Effect of cationic drugs on the transporting activity of human and rat OCT/Oct 1–3 and implications for drug–drug interactions. Xenobiotica 38:9, pages 1203-1218.
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K.-I. Umehara, T. Iwatsubo, K. Noguchi & H. Kamimura. (2007) Functional involvement of organic cation transporter1 (OCT1/Oct1) in the hepatic uptake of organic cations in humans and rats. Xenobiotica 37:8, pages 818-831.
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Articles from other publishers (33)

Stephen H. Wright & Timothy W. Secomb. (2022) Novel method for kinetic analysis applied to transport by the uniporter OCT2. American Journal of Physiology-Renal Physiology 323:3, pages F370-F387.
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Bastian Haberkorn, Martin F. Fromm & Jörg König. (2021) Transport of Drugs and Endogenous Compounds Mediated by Human OCT1: Studies in Single- and Double-Transfected Cell Models. Frontiers in Pharmacology 12.
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Heinz Bönisch. 2021. Organic Cation Transporters in the Central Nervous System. Organic Cation Transporters in the Central Nervous System 119 167 .
Metee Jinakote, Atcharaporn Ontawong, Sunhapas Soodvilai, Jeerawat Pimta, Tipthida Pasachan, Varanuj Chatsudthipong & Chutima Srimaroeng. (2020) High affinity of 4‐(4‐(dimethylamino)styryl)‐ N ‐methylpyridinium transport for assessing organic cation drugs in hepatocellular carcinoma cells . Fundamental & Clinical Pharmacology 34:3, pages 365-379.
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Shoetsu Chiba, Ayako Ro, Toru Ikawa, Yukino Oide & Toshiji Mukai. (2020) Interactions of human organic anion transporters 1–4 and human organic cation transporters 1–3 with the stimulant drug methamphetamine and amphetamine. Legal Medicine 44, pages 101689.
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Philip J. Sandoval, Mark Morales, Timothy W. Secomb & Stephen H. Wright. (2019) Kinetic basis of metformin-MPP interactions with organic cation transporter OCT2. American Journal of Physiology-Renal Physiology 317:3, pages F720-F734.
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V. A. Aleshin, G. V. Mkrtchyan & V. I. Bunik. (2019) Mechanisms of Non-coenzyme Action of Thiamine: Protein Targets and Medical Significance. Biochemistry (Moscow) 84:8, pages 829-850.
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Sungwoo Hyung, Wonji Pyeon, Ji Eun Park, Yoo-Kyung Song & Suk-Jae Chung. (2017) The conditional stimulation of rat organic cation transporter 2, but not its human ortholog, by mesoridazine: the possibility of the involvement of the high-affinity binding site of the transporter in the stimulation. Journal of Pharmacy and Pharmacology 69:11, pages 1513-1523.
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Anton Ivanyuk, Françoise Livio, Jérôme Biollaz & Thierry Buclin. (2017) Renal Drug Transporters and Drug Interactions. Clinical Pharmacokinetics 56:8, pages 825-892.
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Ayman F. El‐Kattan. 2017. Oral Bioavailability Assessment. Oral Bioavailability Assessment 77 138 .
Ulf Schulze, Sabine Brast, Alexander Grabner, Christian Albiker, Beatrice Snieder, Svenja Holle, Eberhard Schlatter, Rita Schröter, Hermann Pavenstädt, Edwin Herrmann, Carsten Lambert, Gilles A. Spoden, Luise Florin, Paul Saftig & Giuliano Ciarimboli. (2016) Tetraspanin CD63 controls basolateral sorting of organic cation transporter 2 in renal proximal tubules. The FASEB Journal 31:4, pages 1421-1433.
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Yingxin Yu, Mengmeng Wang, Kaiqiong Zhang, Dan Yang, Yufang Zhong, Jing An, Bingli Lei & Xinyu Zhang. (2017) The transepithelial transport mechanism of polybrominated diphenyl ethers in human intestine determined using a Caco-2 cell monolayer. Environmental Research 154, pages 93-100.
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Kandatege Wimalasena. 2017. 81 122 .
S Harrach, C Schmidt-Lauber, T Pap, H Pavenstädt, E Schlatter, E Schmidt, W E Berdel, U Schulze, B Edemir, S Jeromin, T Haferlach, G Ciarimboli & J Bertrand. (2016) MATE1 regulates cellular uptake and sensitivity to imatinib in CML patients. Blood Cancer Journal 6:9, pages e470-e470.
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Takahiro Shibayama, Mark Morales, Xiaohong Zhang, Lucy J. Martínez-Guerrero, Alfred Berteloot, Timothy W. Secomb & Stephen H. Wright. (2015) Unstirred Water Layers and the Kinetics of Organic Cation Transport. Pharmaceutical Research 32:9, pages 2937-2949.
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Victoria Hellberg, Caroline Gahm, Wei Liu, Hans Ehrsson, Helge Rask‐Andersen & Göran Laurell. (2015) Immunohistochemical localization of OCT2 in the cochlea of various species. The Laryngoscope 125:9.
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Thomas Ebner, Naoki Ishiguro & Mitchell E. Taub. (2015) The Use of Transporter Probe Drug Cocktails for the Assessment of Transporter-Based Drug–Drug Interactions in a Clinical Setting—Proposal of a Four Component Transporter Cocktail. Journal of Pharmaceutical Sciences 104:9, pages 3220-3228.
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Kelli H. Boxberger, Bruno Hagenbuch & Jed N. Lampe. (2014) Common Drugs Inhibit Human Organic Cation Transporter 1 (OCT1)-Mediated Neurotransmitter Uptake. Drug Metabolism and Disposition 42:6, pages 990-995.
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Yuan Xu, Xian Liu, Shanshan Li, Nannan Zhou, Likun Gong, Cheng Luo, Xiaomin Luo, Mingyue Zheng, Hualiang Jiang & Kaixian Chen. (2013) Combinatorial Pharmacophore Modeling of Organic Cation Transporter 2 (OCT2) Inhibitors: Insights into Multiple Inhibitory Mechanisms. Molecular Pharmaceutics 10:12, pages 4611-4619.
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Ryota Kikuchi, Yanbin Lao, Daniel A.J. Bow, William J. Chiou, Mark E. Andracki, Robert A. Carr, Richard L. Voorman & Sonia M. De Morais. (2013) Prediction of Clinical Drug–Drug Interactions of Veliparib (ABT-888) with Human Renal Transporters (OAT1, OAT3, OCT2, MATE1, and MATE2K). Journal of Pharmaceutical Sciences 102:12, pages 4426-4432.
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I.S. Song, M.K. Choi, W.S. Shim & C.K. Shim. (2013) Transport of organic cationic drugs: Effect of ion-pair formation with bile salts on the biliary excretion and pharmacokinetics. Pharmacology & Therapeutics 138:1, pages 142-154.
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Sophie L. Stocker, Arian Emami Riedmaier, Matthias Schwab & Kathleen M. Giacomini. 2013. Pharmacogenomics of Human Drug Transporters. Pharmacogenomics of Human Drug Transporters 171 208 .
Rajendra S. Kadam, Sunil K. Vooturi & Uday B. Kompella. (2013) RETRACTION: Immunohistochemical and Functional Characterization of Peptide, Organic Cation, Neutral and Basic Amino Acid, and Monocarboxylate Drug Transporters in Human Ocular Tissues. Drug Metabolism and Disposition 41:2, pages 466-474.
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Yurong Lai. 2013. Transporters in Drug Discovery and Development. Transporters in Drug Discovery and Development 455 631 .
Ryan M. PelisYodying Dangprapai, Yaofeng Cheng, Xiaohong Zhang, Jennifer Terpstra & Stephen H. Wright. (2012) Functional significance of conserved cysteines in the human organic cation transporter 2. American Journal of Physiology-Renal Physiology 303:2, pages F313-F320.
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Pedro Cano‐Soldado & Marçal Pastor‐Anglada. (2011) Transporters that translocate nucleosides and structural similar drugs: structural requirements for substrate recognition. Medicinal Research Reviews 32:2, pages 428-457.
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Sumito Ito, Hiroyuki Kusuhara, Miyu Yokochi, Junko Toyoshima, Katsuhisa Inoue, Hiroaki Yuasa & Yuichi Sugiyama. (2012) Competitive Inhibition of the Luminal Efflux by Multidrug and Toxin Extrusions, but Not Basolateral Uptake by Organic Cation Transporter 2, Is the Likely Mechanism Underlying the Pharmacokinetic Drug-Drug Interactions Caused by Cimetidine in the Kidney. Journal of Pharmacology and Experimental Therapeutics 340:2, pages 393-403.
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J.P. Keogh. 2012. Current Concepts in Drug Metabolism and Toxicology. Current Concepts in Drug Metabolism and Toxicology 1 42 .
Sabine Klatt, Martin F. Fromm & Jörg König. (2011) Transporter-Mediated Drug–Drug Interactions with Oral Antidiabetic Drugs. Pharmaceutics 3:4, pages 680-705.
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Tsuyoshi Minematsu, Megumi Iwai, Ken-ichi Umehara, Takashi Usui & Hidetaka Kamimura. (2010) Characterization of Human Organic Cation Transporter 1 (OCT1/SLC22A1)- and OCT2 (SLC22A2)-Mediated Transport of 1-(2-Methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)- 4,9-dihydro-1 H -naphtho[2,3- d ]imidazolium Bromide (YM155 Monobromide), a Novel Small Molecule Survivin Suppressant . Drug Metabolism and Disposition 38:1, pages 1-4.
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Ken-ichi Umehara, Nobuaki Shirai, Takafumi Iwatsubo, Kiyoshi Noguchi, Takashi Usui & Hidetaka Kamimura. (2009) Identification of Human Metabolites of (–)- N -{2-[( R )-3-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide (YM758), a Novel If Channel Inhibitor, and Investigation of the Transporter-Mediated Renal and Hepatic Excretion of These Metabolites . Drug Metabolism and Disposition 37:8, pages 1646-1657.
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Ken-ichi Umehara, Megumi Iwai, Yasuhisa Adachi, Takafumi Iwatsubo, Takashi Usui & Hidetaka Kamimura. (2008) Hepatic Uptake and Excretion of (–)- N -{2-[( R )-3-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide (YM758), a Novel If Channel Inhibitor, in Rats and Humans . Drug Metabolism and Disposition 36:6, pages 1030-1038.
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K-I Umehara, T Iwatsubo, K Noguchi & H Kamimura. (2008) Functional Involvement of the Organic Cation Transporter 2 (rOct2) in the Renal Uptake of Organic Cations in Rats. Journal of International Medical Research 36:1, pages 123-136.
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