Fluorescent reporters of monoamine transporter distribution and function

Sharanappa M. Bagale, Adrienne S. Brown, Melissa M. Carballosa Gonzalez, Alberto Vitores, Teresa L. Micotto, N. S. Saleesh Kumar, Ian D. Hentall, James N. Wilson

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

Serotonin is a monoamine serving as a chemical messenger in diverse brain regions, as well as in blood and various other organs. We synthesized six ethylamine functionalized fluorophores as fluorescent probes for serotonin. The one with best spectral properties and aqueous solubility, 6-amino-2-(2- aminoethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione, was studied in detail both in vivo and in vitro. It was shown to act as a ligand for serotonin transporter (SERT) without acute cerebral or cardiovascular toxicity or adverse effects. Fluorescent serotonin analogs can be used for direct visualization of SERT distribution and activity in live tissue.

Original languageEnglish (US)
Pages (from-to)7387-7391
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number24
DOIs
StatePublished - Dec 15 2011

Keywords

  • Fluorescent analogs
  • Monoamine transporter
  • Neurotransmitter
  • Reuptake inhibitor
  • Serotonin

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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  • Cite this

    Bagale, S. M., Brown, A. S., Carballosa Gonzalez, M. M., Vitores, A., Micotto, T. L., Saleesh Kumar, N. S., Hentall, I. D., & Wilson, J. N. (2011). Fluorescent reporters of monoamine transporter distribution and function. Bioorganic and Medicinal Chemistry Letters, 21(24), 7387-7391. https://doi.org/10.1016/j.bmcl.2011.10.007