The biogenic amine transporter activity of vinylogous amphetamine analogs
Decker, A., Partilla, J. S., Baumann, M. H., Rothman, R. B., & Blough, B. (2016). The biogenic amine transporter activity of vinylogous amphetamine analogs. MedChemComm, 7, 1657-1663. DOI: 10.1039/C6MD00245E
A series of vinylogous amphetamine analogs was synthesized and examined for their activity at biogenic amine transporters and serotonin-2 receptor (5-HT2) subtypes. (1S,3E)-1-Methyl-4-phenyl-but-3-enylamine (S-6) is a potent dual dopamine/serotonin (DA/5-HT) releaser with no activity at 5-HT2 receptors. This unique profile of actions suggests that analog S-6 is a viable lead compound for identifying new structural classes of DA/5-HT releasers with therapeutic benefit and reduced abuse liability.