ZFIN ID: ZDB-PUB-160802-2
OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity
Rovira, X., Trapero, A., Pittolo, S., Zussy, C., Faucherre, A., Jopling, C., Giraldo, J., Pin, J.P., Gorostiza, P., Goudet, C., Llebaria, A.
Date: 2016
Source: Cell chemical biology   23(8): 929-34 (Journal)
Registered Authors: Faucherre, Adele, Jopling, Chris
Keywords: none
MeSH Terms:
  • Allosteric Regulation/drug effects
  • Allosteric Regulation/radiation effects
  • Animals
  • Azo Compounds/chemistry
  • Azo Compounds/pharmacology*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • HEK293 Cells
  • Humans
  • Light*
  • Mice
  • Mice, Inbred C57BL
  • Pain Threshold/drug effects
  • Pyrrolidonecarboxylic Acid/analogs & derivatives*
  • Pyrrolidonecarboxylic Acid/chemistry
  • Pyrrolidonecarboxylic Acid/pharmacology
  • Receptors, Metabotropic Glutamate/antagonists & inhibitors*
  • Receptors, Metabotropic Glutamate/metabolism
  • Structure-Activity Relationship
  • Time Factors
  • Zebrafish/metabolism
PubMed: 27478159 Full text @ Cell Chem Biol
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.