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Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

AutorFont, Joan; López-Cano, Marc; Notartomaso, Serena; Scarselli, Pamela; Di Pietro, Paola Di; Bresolí-Obach, Roger; Battaglia, Giuseppe; Malhaire, Fanny; Rovira, Xavier; Catena, Juan Lorenzo; Giraldo, Jesús; Pin, Jean Philippe; Fernández-Dueñas, Víctor; Goudet, Cyril; Nonell, Santi; Nicoletti, Ferdinando; Llebaría, Amadeu; Ciruela, Francisco
Palabras clavemGlu5
receptor negative allosteric modulator
Fecha de publicación11-abr-2017
EditoreLife Sciences Publications
CitacióneLife 6: e23545 (2017)
ResumenLight-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type 5 (mGlu5) receptor negative allosteric modulator raseglurant. Violet light illumination of JF-NP-26 induces a photochemical reaction prompting the active-drug’s release, which effectively controls mGlu5 receptor activity both in ectopic expressing systems and in striatal primary neurons. Systemic administration in mice followed by local light-emitting diode (LED)-based illumination, either of the thalamus or the peripheral tissues, induced JF-NP-26-mediated light-dependent analgesia both in neuropathic and in acute/tonic inflammatory pain models. These data offer the first example of optical control of analgesia in vivo using a photocaged mGlu5 receptor negative allosteric modulator. This approach shows potential for precisely targeting, in time and space, endogenous receptors, which may allow a better management of difficult-to-treat disorders. © Font et al.
Versión del editor10.7554/eLife.23545
URIhttp://hdl.handle.net/10261/151772
DOI10.7554/eLife.23545
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