Deborah Rudin, John D McCorvy, Grant C Glatfelter, Dino Luethi, Dániel Szöllősi, Tea Ljubišić, Pierce V Kavanagh, Geraldine Dowling, Marion Holy, Kathrin Jaentsch, Donna Walther, Simon D Brandt, Thomas Stockner, Michael H Baumann, Adam L Halberstadt, Harald H Sitte
Derivatives of (2-aminopropyl)indole (API) and (2-aminopropyl)benzofuran (APB) are new psychoactive substances which produce stimulant effects in vivo. (2-Aminopropyl)benzo[β]thiophene (APBT) is a novel sulfur-based analog of API and APB that has not been pharmacologically characterized. In the current study, we assessed the pharmacological effects of six APBT positional isomers in vitro, and three of these isomers (3-APBT, 5-APBT, and 6-APBT) were subjected to further investigations in vivo. Uptake inhibition and efflux assays in human transporter-transfected HEK293 cells and in rat brain synaptosomes revealed that APBTs inhibit monoamine reuptake and induce transporter-mediated substrate release...
March 2022: Neuropsychopharmacology