OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu 4 Receptor Activity

descriptionPublicationkeyboard_double_arrow_right Article 01 Aug 2016 Spain English Publisher:Elsevier BVJournal:Cell Chemical Biology, volume 23, pages 929-934 (issn: 2451-9456,

Copyright policy )Funded by:EC | OPTICALBULLET, EC | THERALIGHT, EC | HBP SGA2 +3 projects

Authors: Rovira, Xavier; Trapero, Ana; Pittolo, Silvia; Zussy, Charleine; Faucherre, Adèle; Jopling, Chris; Giraldo, Jesús; +4 Authors

doi: 10.1016/j.chembiol.2016.06.013

pmid: 27478159

handle: 10261/177707 , 2445/156117

OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu 4 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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Keywords

Nervous system, Pain Threshold, Time Factors, Light, Chronic pain, OptoGluNAM4.1, Receptors, Metabotropic Glutamate, Mice, Structure-Activity Relationship, Allosteric Regulation, Animals, Humans, Sistema nerviós, Zebrafish, Azobenzene, Dose-Response Relationship, Drug, mGlu receptor, Dolor crònic, Pyrrolidonecarboxylic Acid, Mice, Inbred C57BL, Disease Models, Animal, HEK293 Cells, Schizophrenia, Azo Compounds

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