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https://hdl.handle.net/2445/122570
Título: | Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator |
Autor: | 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 |
Materia: | Neurociències Ratolins (Animals de laboratori) Farmacologia Tractament del dolor Neurosciences Mice (Laboratory animals) Pharmacology Pain treatment |
Fecha de publicación: | 11-abr-2017 |
Publicado por: | eLife Sciences |
Resumen: | 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. |
Nota: | Reproducció del document publicat a: https://doi.org/10.7554/eLife.23545 |
Es parte de: | eLife, 2017, vol. 6, p. e23545 |
URI: | https://hdl.handle.net/2445/122570 |
Recurso relacionado: | https://doi.org/10.7554/eLife.23545 |
ISSN: | 2050-084X |
Aparece en las colecciones: | Articles publicats en revistes (Patologia i Terapèutica Experimental) Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL)) |
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