Oct 6 transporter. Organic cation transporters (OCT) are electrogenic, Na + -independent and reversible. This changed after the discovery of mammalian drug efflux transporters of the ATP-binding cassette (ABC) family, such as Apr 26, 2021 · First, it is proposed which OCT should be tested in vitro. The organic cation/carnitine transporter novel 1 and 2 (OCTN1 and N2) and the organic cation transporter 6 (OCT6) are encoded by the SLC22A4, - 5, and - 16, respectively [3]. This family of proteins can also transport zwitterions and anions, though it is a different subfamily of solute carrier proteins than the organic anion transporters. In the kidney, human organic cation transporters (OCTs) and multidrug and toxin extrusion proteins (MATEs) are the major transporters for the secretion of cationic drugs into the urine. The human organic cation uptake transporter OCT1, encoded by the SLC22A1 gene, is highly expressed in the liver and reported to possess a broad substrate specificity. Interested in FDA or EMA Compliant Transporter Studies? OCT1 (organic cation transporter 1) Aliases: HOCT1, oct1_cds Gene name: Solute carrier family 22 member 1 (SLC22A1) Summary OCT1 is primarily a hepatic uptake transporter, expressed on the sinusoidal membrane (blood side) of hepatocytes. Until recently the role of transporters during reabsorption and excretion of drugs received only minor attention. g. This includes detailed proposals for experimental procedures and minimal requirements for test conditions. anticancer and antihypertension drugs, HIV protease inhibitors, statins, bile acids, bilirubin, prostaglandins, antibiotics and steroids) into and out of the kidney, liver, brain, intestine, placenta and testis. OATPs comprise six members (OATP1–6) of the SLCO gene family that transport anionic, cationic, neutral and zwitterionic compounds (e. Using OCT2 biomarkers and . Recent findings revealed that OCT1 can mediate t … OCT3 (organic cation transporter 3) Aliases: EMT, EMTH Gene name: Solute carrier family 22 member 3 (SLC22A3) Summary OCT3 is an uptake transporter with widespread tissue distribution. These proteins are members of the solute carrier family, subfamily 22. It plays a key role in the disposition and hepatic clearance of mostly cationic drugs and endogenous Organic cation transporter (OCT) 2 and cyclo (His–Pro) transport To exert a functional effect, cyclo (His–Pro) must first be internalised by cells. They transport organic cations, zwitterions, and some uncharged compounds and operate as facilitated diffusion systems and/or antiporters. OCTs are critically involved in intestinal absorption, hepatic uptake, and renal excretion of hydrophilic drugs. This article offers a comprehensive overview of the tissue distribution, interspecies differences, and factors affecting its activity—critical for evaluating tissue toxicity and systemic exposure to cationic substances. Second, it is suggested which measurements should be performed with each transporter before a phase 1 clinical trial is started. Indeed, organic cation transporter (OCT)2 is the initial step in the renal secretion of organic cations and consequently plays a defining Mar 1, 2025 · Organic cation transporter 2 (OCT2) is essential for the active tubular secretion of xenobiotics and endogenous cationic substances in the kidneys. Although it is a polyspecific transporter of mainly cationic molecules, and it is expressed in the liver and the kidney, it is not considered as important as OCT1 (liver) and OCT2 (kidney) in the respective Organic cation transporters play a critical role in mediating the distribution of cationic pharmaceuticals. OCT1 operates by facilitated diffusion and allows the entry of nutrients into cells. This review, unlike other reviews that focus on a single transporter family, briefly summarizes the current knowledge of all the functionally characterized human organic anion and cation drug uptake transporters of the SLCO and the SLC22A superfamilies. 0hk jq qthb 3apev 5febvoigc hi8hh yxholqv coyyj ezlwvlz nz13sz