Literature DB >> 25193229

Alpha-ethyltryptamines as dual dopamine-serotonin releasers.

Bruce E Blough1, Antonio Landavazo2, John S Partilla3, Ann M Decker2, Kevin M Page2, Michael H Baumann3, Richard B Rothman3.   

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  5-HT 2A receptor; 5-HT releasers; DA releasers; Tryptamines

Mesh：

Substances：

Year:  2014        PMID： 25193229      PMCID： PMC4211607          DOI： 10.1016/j.bmcl.2014.07.062

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


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