Alpha-ethyltryptamines as dual dopamine-serotonin releasers

Bruce E. Blough; Antonio Landavazo; Ann Marie Decker; Bruce E. Blough; Antonio Landavazo; JS Partilla; Ann Decker; Kevin Page; MH Baumann; RB Rothman

Alpha-ethyltryptamines as dual dopamine-serotonin releasers

Blough, B., Landavazo, A., Partilla, JS., Decker, A., Page, K., Baumann, MH., & Rothman, RB. (2014). Alpha-ethyltryptamines as dual dopamine-serotonin releasers. Bioorganic and Medicinal Chemistry Letters, 24(19), 4754-4758. https://doi.org/10.1016/j.bmcl.2014.07.062

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Abstract

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