Cell Chemical Biology
Volume 23, Issue 8, 18 August 2016, Pages 929-934
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Brief Communication
OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity

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Highlights

  • OptoGluNAM4.1 is an azobenzene active as negative allosteric modulator of mGlu4

  • OptoGluNAM4.1 is isomerized with blue-light/dark cycles with fast relaxation

  • In vivo, OptoGluNAM4.1 regulates the zebrafish embryo motility with light

  • OptoGluNAM4.1 mGlu4 activity is effective in a pain mouse model

Summary

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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