Cellular Uptake of Psychostimulants – Are High- and Low-Affinity Organic Cation Transporters Drug Traffickers?
Frontiers in Pharmacology January 20, 2021 Ole Jensen, Muhammad Rafehi, Lukas Gebauer et al. 24 citations
Several psychostimulants and hallucinogens are transported by organic cation transporters (OCTs), which may contribute to individual differences in their metabolism and toxicity. Mescaline is strongly transported by OCT1, with transport varying substantially across common genetic variants: reduced in variants *2, *3, *4, *5, *6, and moderately increased in *8. Other substances—methamphetamine, para-methoxymethamphetamine, (-)-ephedrine, cathine, and dimethyltryptamine—are substrates of OCT2, with affinities and transport capacities reduced by up to half in the A270S variant. Cathine also acts as a substrate for NET and DAT. These findings suggest that genetic variation in OCTs could underlie highly variable adverse reactions to mescaline and other psychostimulants.