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OCT - Organic cation transporters

Organic cation transporters (OCTs) are members of the solute carrier (SLC) gene family SLC22A acting like OATPs and OATs as multi-specific uptake transporters and expressed in several epithelial membranes in different organs of the body (e.g. liver, intestine, kidney, heart, placenta).

OCTs consist of 12 transmembrane domains and mediate the passive facilitated diffusion of several organic cations alongside their electrochemical gradients. Substrates are structurally unrelated small organic cations, including endogenous and exogenous substrates and many drugs (e.g. creatinine, dopamine, progesterone, anesthetic drugs like ketamine, anticancer drugs like cisplatine and many more.

Although the OCT-mediated transport is independent of the pH value, affinity for several substrates like ketamine does depend on their degree of ionization, leading to an increased transport rate of those substrates at reduced pH values. Genetic variants of OCTs might result in a change of bioavailability of drugs leading to possible severe side effects and/or drug-drug interaction (DDIs).

In cooperation with the University Medicine of Greifswald, Department of Clinical Pharmacology, Primacyt is offering a broad range of stable transfected HEK293 and MDCK2 cells expressing human OCTs. All cells are validated for expression rates, localization of the overexpressed transporter protein and functionality. We analyse uptake functions by using suitable substrates and reference inhibitors.