Design, Synthesis, and In Vitro Characterization of a Tryptamine-Based Visible-Light Photoswitchable 5-HT2AR Ligand Showing Efficacy Preference for β-Arrestin over Mini-Gq.

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Title: Design, Synthesis, and In Vitro Characterization of a Tryptamine-Based Visible-Light Photoswitchable 5-HT2AR Ligand Showing Efficacy Preference for β-Arrestin over Mini-Gq.
Authors: Sink A; Institut für Pharmazie und Lebensmittelchemie, Pharmazeutische und Medizinische Chemie, Julius-Maximilians-Universität Würzburg (JMU), Am Hubland, Würzburg 97074 Germany., Pottie E; Laboratory of Toxicology, Department of Bioanalysis, Faculty of Pharmaceutical Sciences, Ghent University, Ghent B-9000, Belgium., Carter SJ; Department of Chemistry, University of California, Davis, One Shields Avenue, Davis, California 95616, United States.; Institute for Psychedelics and Neurotherapeutics, University of California, Davis, Davis, California 95616, United States., Tombari RJ; Chemistry and Chemical Biology Graduate Program, University of California, Davis, Davis, California 95616, United States., Weber V; Institute for Neuroscience and Medicine (INM-9), Computational Biomedicine, Forschungszentrum Jülich, Wilhelm-Johnen-Straße, Jülich 52425, Germany.; Department of Chemistry, Faculty of Mathematics, Computer Science and Natural Sciences, RWTH Aachen University institution, Aachen 52062, Germany., Carloni P; Institute for Neuroscience and Medicine (INM-9), Computational Biomedicine, Forschungszentrum Jülich, Wilhelm-Johnen-Straße, Jülich 52425, Germany.; Department of Physics, Faculty of Mathematics, Computer Science and Natural Sciences, RWTH Aachen University, Aachen 52062, Germany., Rossetti G; Institute for Neuroscience and Medicine (INM-9), Computational Biomedicine, Forschungszentrum Jülich, Wilhelm-Johnen-Straße, Jülich 52425, Germany.; Jülich Supercomputing Center, Forschungszentrum Jülich, Wilhelm-Johnen-Straße, Jülich 52425, Germany.; Department of Neurology, University Hospital Aachen, RWTH Aachen University, Pauwelsstraße 30, Aachen 52074, Germany., Olson DE; Department of Chemistry, University of California, Davis, One Shields Avenue, Davis, California 95616, United States.; Institute for Psychedelics and Neurotherapeutics, University of California, Davis, Davis, California 95616, United States.; Department of Biochemistry & Molecular Medicine, School of Medicine, University of California, Davis, 2700 Stockton Blvd, Suite 2102, Sacramento, California 95817, United States.; Center for Neuroscience, University of California, Davis, 1544 Newton Ct, Davis, California 95618, United States., Stove CP; Laboratory of Toxicology, Department of Bioanalysis, Faculty of Pharmaceutical Sciences, Ghent University, Ghent B-9000, Belgium., Decker M; Institut für Pharmazie und Lebensmittelchemie, Pharmazeutische und Medizinische Chemie, Julius-Maximilians-Universität Würzburg (JMU), Am Hubland, Würzburg 97074 Germany.
Source: Journal of medicinal chemistry [J Med Chem] 2025 Jul 10; Vol. 68 (13), pp. 13628-13639. Date of Electronic Publication: 2025 Jun 18.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.5c00442