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Literature DB >> 32275382

A Photoswitchable Inhibitor of the Human Serotonin Transporter.

Bichu Cheng^1,2, Johannes Morstein², Lucy Kate Ladefoged³, Jannick Bang Maesen⁴, Birgit Schiøtt³, Steffen Sinning⁴, Dirk Trauner².

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.

Entities: Chemical

Keywords: Photopharmacology; neurotransmitter; photochromic ligand; serotonin; transporter

Mesh：

Substances：

Year: 2020 PMID： 32275382 PMCID： PMC8022892 DOI： 10.1021/acschemneuro.9b00521

Source DB: PubMed Journal: ACS Chem Neurosci ISSN： 1948-7193 Impact factor: 4.418

38 in total

1. AzoCholine Enables Optical Control of Alpha 7 Nicotinic Acetylcholine Receptors in Neural Networks.

Authors: Arunas Damijonaitis; Johannes Broichhagen; Tatsuya Urushima; Katharina Hüll; Jatin Nagpal; Laura Laprell; Matthias Schönberger; David H Woodmansee; Amir Rafiq; Martin P Sumser; Wolfgang Kummer; Alexander Gottschalk; Dirk Trauner
Journal: ACS Chem Neurosci Date: 2015-03-27 Impact factor: 4.418

2. Photoswitchable Inhibitor of a Glutamate Transporter.

Authors: Bichu Cheng; Denis Shchepakin; Michael P Kavanaugh; Dirk Trauner
Journal: ACS Chem Neurosci Date: 2017-05-16 Impact factor: 4.418

3. A photochromic agonist for μ-opioid receptors.

Authors: Matthias Schönberger; Dirk Trauner
Journal: Angew Chem Int Ed Engl Date: 2014-02-12 Impact factor: 15.336

Review 4. Azobenzene photoswitches for biomolecules.

Authors: Andrew A Beharry; G Andrew Woolley
Journal: Chem Soc Rev Date: 2011-04-12 Impact factor: 54.564

5. Characterization of an allosteric citalopram-binding site at the serotonin transporter.

Authors: Fenghua Chen; Mads Breum Larsen; Henrik Amtoft Neubauer; Connie Sánchez; Per Plenge; Ove Wiborg
Journal: J Neurochem Date: 2005-01 Impact factor: 5.372

6. Future directions for serotonin and antidepressants.

Authors: Francesc Artigas
Journal: ACS Chem Neurosci Date: 2013-01-16 Impact factor: 4.418

7. Steric hindrance mutagenesis in the conserved extracellular vestibule impedes allosteric binding of antidepressants to the serotonin transporter.

Authors: Per Plenge; Lei Shi; Thijs Beuming; Jerez Te; Amy Hauck Newman; Harel Weinstein; Ulrik Gether; Claus J Loland
Journal: J Biol Chem Date: 2012-09-24 Impact factor: 5.157

A Photoswitchable Inhibitor of the Human Serotonin Transporter.

1. AzoCholine Enables Optical Control of Alpha 7 Nicotinic Acetylcholine Receptors in Neural Networks.

2. Photoswitchable Inhibitor of a Glutamate Transporter.

3. A photochromic agonist for μ-opioid receptors.

Review 4. Azobenzene photoswitches for biomolecules.

5. Characterization of an allosteric citalopram-binding site at the serotonin transporter.

6. Future directions for serotonin and antidepressants.

7. Steric hindrance mutagenesis in the conserved extracellular vestibule impedes allosteric binding of antidepressants to the serotonin transporter.

8. Photoswitchable fatty acids enable optical control of TRPV1.

9. Mapping the Azolog Space Enables the Optical Control of New Biological Targets.

10. Photoswitchable diacylglycerols enable optical control of protein kinase C.

Review 1. Molecular photoswitches in aqueous environments.

2. Hypothesis-Driven, Structure-Based Design in Photopharmacology: The Case of eDHFR Inhibitors.

Review 3. Optical control of purinergic signaling.