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urn:hdl:2445/122570 Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator Font, Joan López-Cano, Marc Notartomaso, Serena Scarselli, Pamela Di Pietro, Paola Bresolí-Obach, Roger Battaglia, Giuseppe Malhaire, Fanny Rovira, Xavier Catena, Juanlo Giraldo, Jesús Pin, Jean-Philippe Fernández Dueñas, Víctor Goudet, Cyril Nonell, Santi Nicoletti, Ferdinando Llebaria Soldevila, Amadeu Ciruela Alférez, Francisco Neurociències Ratolins (Animals de laboratori) Farmacologia Tractament del dolor Neurosciences Mice (Laboratory animals) Pharmacology Pain treatment Light-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. 2018-05-25T07:57:00Z 2018-05-25T07:57:00Z 2017-04-11 2018-05-25T07:57:00Z info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion Reproducció del document publicat a: https://doi.org/10.7554/eLife.23545 eLife, 2017, vol. 6, p. e23545 https://doi.org/10.7554/eLife.23545 cc-by (c) Font, Joan et al., 2017 http://creativecommons.org/licenses/by/3.0/es info:eu-repo/semantics/openAccess eLife Sciences Articles publicats en revistes (Patologia i Terapèutica Experimental)