title: OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity.
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.
authors.affiliation: Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, 34000 Montpellier, France; INSERM, U1191, 34000 Montpellier, France.
authors.forename: Xavier
authors.initials: X
authors.lastname: Rovira
authors.affiliation: Laboratory of Medicinal Chemistry, Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), 08034 Barcelona, Spain; Institute for Bioengineering of Catalonia (IBEC), 08028 Barcelona, Spain.
authors.forename: Ana
authors.initials: A
authors.lastname: Trapero
authors.affiliation: Institute for Bioengineering of Catalonia (IBEC), 08028 Barcelona, Spain.
authors.forename: Silvia
authors.initials: S
authors.lastname: Pittolo
authors.affiliation: Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, 34000 Montpellier, France; INSERM, U1191, 34000 Montpellier, France.
authors.forename: Charleine
authors.initials: C
authors.lastname: Zussy
authors.affiliation: Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, 34000 Montpellier, France; INSERM, U1191, 34000 Montpellier, France.
authors.forename: Adèle
authors.initials: A
authors.lastname: Faucherre
authors.affiliation: Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, 34000 Montpellier, France; INSERM, U1191, 34000 Montpellier, France.
authors.forename: Chris
authors.initials: C
authors.lastname: Jopling
authors.affiliation: Laboratory of Molecular Neuropharmacology and Bioinformatics, Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain.
authors.forename: Jesús
authors.initials: J
authors.lastname: Giraldo
authors.affiliation: Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, 34000 Montpellier, France; INSERM, U1191, 34000 Montpellier, France.
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Pin
authors.affiliation: 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.
authors.forename: Pau
authors.initials: P
authors.lastname: Gorostiza
authors.affiliation: 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.
authors.forename: Cyril
authors.initials: C
authors.lastname: Goudet
authors.affiliation: Laboratory of Medicinal Chemistry, Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), 08034 Barcelona, Spain. Electronic address: amadeu.llebaria@iqac.csic.es.
authors.forename: Amadeu
authors.initials: A
authors.lastname: Llebaria
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects / Q000528:radiation effects; D000818:Animals; D001391:Azo Compounds / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D008027:Light; D051379:Mice; D008810:Mice, Inbred C57BL; D017288:Pain Threshold / Q000187:drug effects; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013997:Time Factors; D015027:Zebrafish / Q000378:metabolism
chemical_list: D001391:Azo Compounds; C000624706:OptoGluNAM4.1; D018094:Receptors, Metabotropic Glutamate; D011761:Pyrrolidonecarboxylic Acid; C108823:metabotropic glutamate receptor 4