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- W4206030661 abstract "Serotonin receptors play central roles in neuromodulation and are critical drug targets for psychiatric disorders. Optical control of serotonin receptor subtypes has the potential to greatly enhance our understanding of the spatiotemporal dynamics of receptor function. While other neuromodulatory receptors have been successfully rendered photoswitchable, reversible photocontrol of serotonin receptors has not been achieved, representing a major gap in GPCR photopharmacology. Herein, we develop the first tools that allow for such control. Azo5HT-2 shows light-dependent 5-HT2A R agonism, with greater activity in the cis-form. Based on docking and test compound analysis, we also develop photoswitchable orthogonal, remotely-tethered ligands (PORTLs). These BG-Azo5HTs provide rapid, reversible, and repeatable optical control following conjugation to SNAP-tagged 5-HT2A R. Overall, this study provides a foundation for the broad extension of photopharmacology to the serotonin receptor family." @default.
- W4206030661 created "2022-01-26" @default.
- W4206030661 creator A5031211334 @default.
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- W4206030661 date "2022-03-07" @default.
- W4206030661 modified "2023-10-16" @default.
- W4206030661 title "Photoswitchable Serotonins for Optical Control of the 5‐HT<sub>2A</sub> Receptor**" @default.
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- W4206030661 doi "https://doi.org/10.1002/anie.202117094" @default.
- W4206030661 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34989082" @default.
- W4206030661 hasPublicationYear "2022" @default.
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