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Alpha-ethyltryptamines as dual dopamine-serotonin releasers.

Blough, Bruce E; Landavazo, Antonio; Partilla, John S; Decker, Ann M; Page, Kevin M; Baumann, Michael H; Rothman, Richard B.
Bioorg Med Chem Lett; 24(19): 4754-4758, 2014 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-25193229
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.
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