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. 2014 Oct 1;24(19):4754-4758.
doi: 10.1016/j.bmcl.2014.07.062. Epub 2014 Jul 29.

Alpha-ethyltryptamines as dual dopamine-serotonin releasers

Bruce E Blough  1 , Antonio Landavazo  2 , John S Partilla  3 , Ann M Decker  2 , Kevin M Page  2 , Michael H Baumann  3 , Richard B Rothman  3
Affiliations

Alpha-ethyltryptamines as dual dopamine-serotonin releasers

Bruce E Blough et al. Bioorg Med Chem Lett. .

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.

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

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Figures

Scheme 1
Scheme 1
Synthesis of tryptamine analogs.
Scheme 2
Scheme 2
Synthesis of α-alkylated tryptamine analogs.
Scheme 3
Scheme 3
Synthesis of optically-active tryptamine analogs.
See this image and copyright information in PMC

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