• Article

Alpha-ethyltryptamines as dual dopamine-serotonin releasers


Blough, B., Landavazo, A., Partilla, J. S., Decker, A., Page, K., Baumann, M. H., & Rothman, R. B. (2014). Alpha-ethyltryptamines as dual dopamine-serotonin releasers. Bioorganic and Medicinal Chemistry Letters, 24(19), 4754-4758. DOI: 10.1016/j.bmcl.2014.07.062


The dopamine (DA), serotonin (5-HT), and norepinephrine (NE) transporter releasing activity and serotonin-2A (5-HT2A) receptor agonist activity of a series of substituted tryptamines are reported. Three compounds, 7b, (+)-7d and 7f, were found to be potent dual DA/5-HT releasers and were >10-fold less potent as NE releasers. Additionally, these compounds had different activity profiles at the 5-HT2A receptor. The unique combination of dual DA/5-HT releasing activity and 5-HT2A receptor activity suggests that these compounds could represent a new class of neurotransmitter releasers with therapeutic potential