2026-04-13T02:23:24Zhttps://recercat.cat/oai/request

oai:recercat.cat:2445/1225702025-12-05T12:32:09Zcom_2072_1057col_2072_478916col_2072_478917col_2072_478929

00925njm 22002777a 4500 dc Font, Joan author López-Cano, Marc author Notartomaso, Serena author Scarselli, Pamela author Di Pietro, Paola author Bresolí-Obach, Roger author Battaglia, Giuseppe author Malhaire, Fanny author Rovira, Xavier author Catena, Juanlo author Giraldo, Jesús author Pin, Jean-Philippe author Fernández Dueñas, Víctor author Goudet, Cyril author Nonell, Santi author Nicoletti, Ferdinando author Llebaria Soldevila, Amadeu author Ciruela Alférez, Francisco author 2018-05-25T07:57:00Z 2018-05-25T07:57:00Z 2017-04-11 2018-05-25T07:57:00Z 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. Neurociències Ratolins (Animals de laboratori) Farmacologia Tractament del dolor Neurosciences Mice (Laboratory animals) Pharmacology Pain treatment Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator