| 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: |
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| PubMed: | 27478159 Full text @ Cell Chem Biol |
Citation
Rovira, X., Trapero, A., Pittolo, S., Zussy, C., Faucherre, A., Jopling, C., Giraldo, J., Pin, J.P., Gorostiza, P., Goudet, C., Llebaria, A. (2016) OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity. Cell chemical biology. 23(8):929-34.
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.
ADDITIONAL INFORMATION
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