Alpha-ethyltryptamines as dual dopamine-serotonin releasers

  • Bioorg Med Chem Lett. 2014 Oct 1;24(19):4754-4758. doi: 10.1016/j.bmcl.2014.07.062.
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
  • 1. Center for Drug Discovery, Research Triangle Institute, 3040 Cornwallis Road, Research Triangle Park, NC 27709, USA. Electronic address: [email protected].
  • 2. Center for Drug Discovery, Research Triangle Institute, 3040 Cornwallis Road, Research Triangle Park, NC 27709, USA.
  • 3. Medicinal Chemistry Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA.
PMID: 25193229 DOI: 10.1016/j.bmcl.2014.07.062
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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