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

Xavier Rovira, Ana Trapero, Silvia Pittolo, Charleine Zussy, Adèle Faucherre, Chris Jopling, Jesús Giraldo, Jean Philippe Pin, Pau Gorostiza, Cyril Goudet, Amadeu Llebaria

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)

Abstract

© 2016 Elsevier Ltd 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.
Original languageEnglish
Pages (from-to)929-934
JournalCell Chemical Biology
Volume23
Issue number8
DOIs
Publication statusPublished - 18 Aug 2016

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