scholarly journals Role of Human Organic Cation Transporter 1 (hOCT1) Polymorphisms in Lamivudine (3TC) Uptake and Drug-Drug Interactions

2016 ◽  
Vol 7 ◽  
Author(s):  
Cristina Arimany-Nardi ◽  
Gerard Minuesa ◽  
Thorsten Keller ◽  
Itziar Erkizia ◽  
Hermann Koepsell ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Organic Cation ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 1

scholarly journals OCTN1: A Widely Studied but Still Enigmatic Organic Cation Transporter Linked to Human Pathology and Drug Interactions

2022 ◽  
Vol 23 (2) ◽  
pp. 914
Author(s):  
Lorena Pochini ◽  
Michele Galluccio ◽  
Mariafrancesca Scalise ◽  
Lara Console ◽  
Gilda Pappacoda ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Functional Role ◽  
Organic Cation ◽  
Tertiary Structure ◽  
Organic Cation Transporter ◽  
Tissue Expression ◽  
Functional Studies ◽  
Experimental Systems ◽  
Human Pathology

The Novel Organic Cation Transporter, OCTN1, is the first member of the OCTN subfamily; it belongs to the wider Solute Carrier family SLC22, which counts many members including cation and anion organic transporters. The tertiary structure has not been resolved for any cation organic transporter. The functional role of OCNT1 is still not well assessed despite the many functional studies so far conducted. The lack of a definitive identification of OCTN1 function can be attributed to the different experimental systems and methodologies adopted for studying each of the proposed ligands. Apart from the contradictory data, the international scientific community agrees on a role of OCTN1 in protecting cells and tissues from oxidative and/or inflammatory damage. Moreover, the involvement of this transporter in drug interactions and delivery has been well clarified, even though the exact profile of the transported/interacting molecules is still somehow confusing. Therefore, OCTN1 continues to be a hot topic in terms of its functional role and structure. This review focuses on the most recent advances on OCTN1 in terms of functional aspects, physiological roles, substrate specificity, drug interactions, tissue expression, and relationships with pathology.

scholarly journals Reduced Hepatic Uptake and Intestinal Excretion of Organic Cations in Mice with a Targeted Disruption of the Organic Cation Transporter 1 (Oct1 [Slc22a1]) Gene

2001 ◽  
Vol 21 (16) ◽  
pp. 5471-5477 ◽  
Author(s):  
Johan W. Jonker ◽  
Els Wagenaar ◽  
Carla A. A. M. Mol ◽  
Marije Buitelaar ◽  
Hermann Koepsell ◽  
...  
Keyword(s):  
Organic Cation ◽  
Basolateral Membrane ◽  
Organic Cation Transporter ◽  
Hepatic Uptake ◽  
Organic Cations ◽  
Wild Type ◽  
Targeted Disruption ◽  
Intestinal Excretion ◽  
Organic Cation Transporter 1

ABSTRACT The polyspecific organic cation transporter 1 (OCT1 [SLC22A1]) mediates facilitated transport of small (hydrophilic) organic cations. OCT1 is localized at the basolateral membrane of epithelial cells in the liver, kidney, and intestine and could therefore be involved in the elimination of endogenous amines and xenobiotics via these organs. To investigate the pharmacologic and physiologic role of this transport protein, we generated Oct1 knockout (Oct1 −/−) mice.Oct1 −/− mice appeared to be viable, healthy, and fertile and displayed no obvious phenotypic abnormalities. The role of Oct1 in the pharmacology of substrate drugs was studied by comparing the distribution and excretion of the model substrate tetraethylammonium (TEA) after intravenous administration to wild-type and Oct1 −/− mice. InOct1 −/− mice, accumulation of TEA in liver was four to sixfold lower than in wild-type mice, whereas direct intestinal excretion of TEA was reduced about twofold. Excretion of TEA into urine over 1 h was 53% of the dose in wild-type mice, compared to 80% in knockout mice, probably because inOct1 −/− mice less TEA accumulates in the liver and thus more is available for rapid excretion by the kidney. In addition, we found that absence of Oct1 leads to decreased liver accumulation of the anticancer drug metaiodobenzylguanidine and the neurotoxin 1-methyl-4-phenylpyridium. In conclusion, our data show that Oct1 plays an important role in the uptake of organic cations into the liver and in their direct excretion into the lumen of the small intestine.

scholarly journals Role of Organic Cation Transporter 1, OCT1 in the Pharmacokinetics and Toxicity of cis-Diammine(pyridine)chloroplatinum(II) and Oxaliplatin in Mice

2010 ◽  
Vol 28 (3) ◽  
pp. 610-625 ◽  
Author(s):  
Shuanglian Li ◽  
Ying Chen ◽  
Shuzhong Zhang ◽  
Swati S. More ◽  
Xiaozhu Huang ◽  
...  
Keyword(s):  
Organic Cation ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 1

scholarly journals Drug-Drug Interactions at Organic Cation Transporter 1

2021 ◽  
Vol 12 ◽  
Author(s):  
Shiwei Zhou ◽  
Sujuan Zeng ◽  
Yan Shu
Keyword(s):  
Drug Interactions ◽  
Organic Cation ◽  
Organic Cation Transporter ◽  
Vital Role ◽  
Organic Cations ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Organic Cation Transporter 1 ◽  
Solute Carrier ◽  
Endogenous Substances ◽  
Interaction Between Drugs

The interaction between drugs and various transporters is one of the decisive factors that affect the pharmacokinetics and pharmacodynamics of drugs. The organic cation transporter 1 (OCT1) is a member of the Solute Carrier 22A (SLC22A) family that plays a vital role in the membrane transport of organic cations including endogenous substances and xenobiotics. This article mainly discusses the drug-drug interactions (DDIs) mediated by OCT1 and their clinical significance.

L503F variant of carnitine/organic cation transporter 1 efficiently transports metformin and other biguanides

2016 ◽  
Vol 68 (9) ◽  
pp. 1160-1169 ◽  
Author(s):  
Azusa Futatsugi ◽  
Yusuke Masuo ◽  
Shiori Kawabata ◽  
Noritaka Nakamichi ◽  
Yukio Kato
Keyword(s):  
Organic Cation ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 1
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