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Alpha-ethyltryptamines as dual dopamine-serotonin releasers.


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.

SUBMITTER: Blough BE 

PROVIDER: S-EPMC4211607 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature

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Alpha-ethyltryptamines as dual dopamine-serotonin releasers.

Blough Bruce E BE   Landavazo Antonio A   Partilla John S JS   Decker Ann M AM   Page Kevin M KM   Baumann Michael H MH   Rothman Richard B RB  

Bioorganic & medicinal chemistry letters 20140729 19


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  ...[more]

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