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Blough BE, Landavazo A, Partilla JS, et al. Hybrid dopamine uptake blocker-serotonin releaser ligands: a new twist on transporter-focused therapeutics. ACS Med Chem Lett. 2014;5(6):623-7doi: 10.1021/ml500113s.
Blough, B. E., Landavazo, A., Partilla, J. S., Baumann, M. H., Decker, A. M., Page, K. M., & Rothman, R. B. (2014). Hybrid dopamine uptake blocker-serotonin releaser ligands: a new twist on transporter-focused therapeutics. ACS medicinal chemistry letters, 5(6), 623-7. https://doi.org/10.1021/ml500113s
Blough, Bruce E, et al. "Hybrid dopamine uptake blocker-serotonin releaser ligands: a new twist on transporter-focused therapeutics." ACS medicinal chemistry letters vol. 5,6 (2014): 623-7. doi: https://doi.org/10.1021/ml500113s
Blough BE, Landavazo A, Partilla JS, Baumann MH, Decker AM, Page KM, Rothman RB. Hybrid dopamine uptake blocker-serotonin releaser ligands: a new twist on transporter-focused therapeutics. ACS Med Chem Lett. 2014 Apr 15;5(6):623-7. doi: 10.1021/ml500113s. eCollection 2014 Jun 12. PMID: 24944732; PMCID: PMC4060932.
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ACS Med Chem Lett. 2014 Apr 15;5(6):623-7. doi: 10.1021/ml500113s. eCollection 2014 Jun 12.

Hybrid dopamine uptake blocker-serotonin releaser ligands: a new twist on transporter-focused therapeutics.

ACS medicinal chemistry letters

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

Affiliations

  1. Center for Drug Discovery, Discovery-Science-Technology, RTI International , 3040 Cornwallis Road, Research Triangle Park, North Carolina 27709, United States.
  2. Medicinal Chemistry Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health , Baltimore, Maryland 21224, United States.

PMID: 24944732 PMCID: PMC4060932 DOI: 10.1021/ml500113s

Abstract

As part of our program to study neurotransmitter releasers, we report herein a class of hybrid dopamine reuptake inhibitors that display serotonin releasing activity. Hybrid compounds are interesting since they increase the design potential of transporter related compounds and hence represent a novel and unexplored strategy for therapeutic drug discovery. A series of N-alkylpropiophenones was synthesized and assessed for uptake inhibition and release activity using rat brain synaptosomes. Substitution on the aromatic ring yielded compounds that maintained hybrid activity, with the two disubstituted analogues (PAL-787 and PAL-820) having the most potent hybrid activity.

Keywords: Dopamine uptake inhibitors; cocaine; methamphetamine; serotonin receptor; serotonin releasers

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