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Title: OptoGluNAM4.1, a Photoswitchable allosteric antagonist for real-time control of mGlu4 receptor activity
Author: Rovira, Xavier
Trapero, Ana
Pittolo, Silvia
Zussy, Charleine
Faucherre, Adèle
Jopling, Chris
Giraldo, Jesús
Pin, Jean-Philippe
Gorostiza Langa, Pablo Ignacio
Goudet, Cyril
Llebaria Soldevila, Amadeu
Keywords: Sistema nerviós
Dolor crònic
Nervous system
Chronic pain
Issue Date: 18-Aug-2016
Publisher: Elsevier
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.
It is part of: Cell Chemical Biology, 2016, vol. 23, num. 8 p. 929-934
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Appears in Collections:Publicacions de projectes de recerca finançats per la UE
Articles publicats en revistes (Institut de Bioenginyeria de Catalunya (IBEC))

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