Neurochemical binding profiles of novel indole and benzofuran MDMA analogues.
Naunyn Schmiedebergs Arch Pharmacol September 20, 2016 Jakob A. Shimshoni, Ilan Winkler, Ezekiel Golan et al. 23 citations
Four MDMA analogues—three benzofuran compounds (5-APB, 6-MAPB, 5-MAPB) and one indole compound (5-IT)—were screened as potential second-generation drugs for PTSD. All analogues showed high binding affinities for serotonin 5-HT2a,b,c and norepinephrine α2 receptors, and significantly inhibited serotonin, dopamine, and norepinephrine uptake. 5-APB acted as an agonist at all three 5-HT2 receptor subtypes, while 6-MAPB, 5-MAPB, and 5-IT were agonists at the 5-HT2c receptor. The analogues also emerged as potent and selective inhibitors of monoamine oxidase A. 6-MAPB, with a favorable pharmacological profile, was further tested for its potency at monoamine transporters. Overall, the analogues displayed higher binding affinities and greater agonist activity at 5-HT2a,c receptors compared to MDMA.