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      OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity.

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          Abstract

          OptoGluNAM4.1, a negative allosteric modulator (NAM) of metabotropic glutamate receptor 4 (mGlu4) contains a reactive group that covalently binds to the receptor and a blue-light-activated, fast-relaxing azobenzene group that allows reversible receptor activity photocontrol in vitro and in vivo. OptoGluNAM4.1 induces light-dependent behavior in zebrafish and reverses the activity of the mGlu4 agonist LSP4-2022 in a mice model of chronic pain, defining a photopharmacological tool to better elucidate the physiological roles of the mGlu4 receptor in the nervous system.

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          Author and article information

          Journal
          Cell Chem Biol
          Cell chemical biology
          Elsevier BV
          2451-9456
          Aug 18 2016
          : 23
          : 8
          Affiliations
          [1 ] Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, 34000 Montpellier, France; INSERM, U1191, 34000 Montpellier, France.
          [2 ] Laboratory of Medicinal Chemistry, Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), 08034 Barcelona, Spain; Institute for Bioengineering of Catalonia (IBEC), 08028 Barcelona, Spain.
          [3 ] Institute for Bioengineering of Catalonia (IBEC), 08028 Barcelona, Spain.
          [4 ] Laboratory of Molecular Neuropharmacology and Bioinformatics, Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain.
          [5 ] Institute for Bioengineering of Catalonia (IBEC), 08028 Barcelona, Spain; Network Biomedical Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Poeta Mariano Esquillor s/n, Zaragoza 50018, Spain; ICREA, Pg. Lluís Companys, 23, Barcelona 08010, Spain. Electronic address: pau@icrea.cat.
          [6 ] Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, 34000 Montpellier, France; INSERM, U1191, 34000 Montpellier, France. Electronic address: cyril.goudet@igf.cnrs.fr.
          [7 ] Laboratory of Medicinal Chemistry, Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), 08034 Barcelona, Spain. Electronic address: amadeu.llebaria@iqac.csic.es.
          Article
          S2451-9456(16)30206-9
          10.1016/j.chembiol.2016.06.013
          27478159
          bea0ec8f-2593-483b-949c-f72cff5d3707
          History

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