OptoGluNAM4.1, a Photoswitchable allosteric antagonist for real-time control of mGlu4 receptor activity

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. Opt...

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Detalles Bibliográficos
Autores: 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
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2016
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/156117
Acceso en línea:https://hdl.handle.net/2445/156117
Access Level:acceso abierto
Palabra clave:Sistema nerviós
Dolor crònic
Nervous system
Chronic pain
Descripción
Sumario: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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