Pharmacological characterization of 3,4-methylenedioxyamphetamine (MDA) analogs and two amphetamine-based compounds: ,α-DEPEA and DPIA
European Neuropsychopharmacology April 1, 2022 Karolina E. Kolaczynska, Paula Ducret, Daniel Trachsel et al. 7 citations
MDA and related amphetamine-based compounds found in street drugs and sport supplements vary in their effects on monoamine transporters and receptors. Most compounds inhibited norepinephrine uptake most potently and preferentially blocked serotonin over dopamine uptake, except 3C-BOH and N,α-DEPEA, which favored dopamine uptake. Several compounds triggered monoamine release, and most bound to serotonin 5-HT2A and 5-HT2C receptors with micromolar affinity, acting as partial or full agonists at 5-HT2A and 5-HT2B. Some also interacted with adrenergic receptors and TAAR1. Fluorinated MDA analogs resembled MDMA's profile, while 3C-BOH and N,α-DEPEA showed amphetamine-like dopaminergic activity. Further pharmacokinetic and pharmacodynamic studies are needed to assess risks and therapeutic potential.