A Photoswitchable Inhibitor of the Human Serotonin Transporter

Bichu Cheng, Johannes Morstein, Lucy Kate Ladefoged, Jannick Bang Maesen, Birgit Schiøtt, Steffen Sinning, Dirk Trauner

Research output: Contribution to journalArticle

Abstract

The human serotonin transporter (hSERT) terminates serotonergic signaling through reuptake of neurotransmitter into presynaptic neurons and is a target for many antidepressant drugs. We describe here the development of a photoswitchable hSERT inhibitor, termed azo-escitalopram, that can be reversibly switched between trans and cis configurations using light of different wavelengths. The dark-adapted trans isomer was found to be significantly less active than the cis isomer, formed upon irradiation.

Original languageEnglish (US)
Pages (from-to)1231-1237
Number of pages7
JournalACS Chemical Neuroscience
Volume11
Issue number9
DOIs
StatePublished - May 6 2020

Keywords

  • Photopharmacology
  • neurotransmitter
  • photochromic ligand
  • serotonin
  • transporter

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Cognitive Neuroscience
  • Cell Biology

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  • Cite this

    Cheng, B., Morstein, J., Ladefoged, L. K., Maesen, J. B., Schiøtt, B., Sinning, S., & Trauner, D. (2020). A Photoswitchable Inhibitor of the Human Serotonin Transporter. ACS Chemical Neuroscience, 11(9), 1231-1237. https://doi.org/10.1021/acschemneuro.9b00521