A Photoswitchable Inhibitor of the Human Serotonin Transporter
Bichu Cheng, Johannes Morstein, Lucy Kate Ladefoged, Jannick Bang Maesen, Birgit Schiøtt, Steffen Sinning, Dirk Trauner
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.
Topics & Concepts
SerotonergicEscitalopramSerotonin transporterSerotoninSerotonin Plasma Membrane Transport ProteinsNeurotransmitterReuptake inhibitorTransporterAntidepressantChemistrySerotonin reuptake inhibitorPharmacologyReuptakeNeurotransmitter transporterNeuroscienceBiochemistryBiologyReceptorGeneHippocampusPhotochromic and Fluorescence ChemistryPhotoreceptor and optogenetics researchRetinal Development and Disorders