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 Hentall, James N Wilson

Research output: Contribution to journalArticle

3 Citations (Scopus)

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

Fingerprint

Serotonin
Serotonin Plasma Membrane Transport Proteins
Fluorophores
Fluorescent Dyes
Solubility
Toxicity
Brain
Blood
Visualization
Tissue
Ligands
ethylamine
isoquinoline
In Vitro Techniques

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

Cite this

Bagale, S. M., Brown, A. S., Carballosa Gonzalez, M. M., Vitores, A., Micotto, T. L., Saleesh Kumar, N. S., ... 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

Fluorescent reporters of monoamine transporter distribution and function. / Bagale, Sharanappa M.; Brown, Adrienne S.; Carballosa Gonzalez, Melissa M.; Vitores, Alberto; Micotto, Teresa L.; Saleesh Kumar, N. S.; Hentall, Ian; Wilson, James N.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 24, 15.12.2011, p. 7387-7391.

Research output: Contribution to journalArticle

Bagale, SM, Brown, AS, Carballosa Gonzalez, MM, Vitores, A, Micotto, TL, Saleesh Kumar, NS, Hentall, I & Wilson, JN 2011, 'Fluorescent reporters of monoamine transporter distribution and function', Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 24, pp. 7387-7391. https://doi.org/10.1016/j.bmcl.2011.10.007
Bagale SM, Brown AS, Carballosa Gonzalez MM, Vitores A, Micotto TL, Saleesh Kumar NS et al. Fluorescent reporters of monoamine transporter distribution and function. Bioorganic and Medicinal Chemistry Letters. 2011 Dec 15;21(24):7387-7391. https://doi.org/10.1016/j.bmcl.2011.10.007
Bagale, Sharanappa M. ; Brown, Adrienne S. ; Carballosa Gonzalez, Melissa M. ; Vitores, Alberto ; Micotto, Teresa L. ; Saleesh Kumar, N. S. ; Hentall, Ian ; Wilson, James N. / Fluorescent reporters of monoamine transporter distribution and function. In: Bioorganic and Medicinal Chemistry Letters. 2011 ; Vol. 21, No. 24. pp. 7387-7391.
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