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2017-04-11

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cc-by (c) Font, Joan et al., 2017
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/122570

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

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Recurs relacionat

https://doi.org/10.7554/eLife.23545

Resum

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.

Matèries

Neurociències, Ratolins (Animals de laboratori), Farmacologia, Tractament del dolor

Matèries (anglès)

Neurosciences, Mice (Laboratory animals), Pharmacology, Pain treatment

Citació

Col·leccions

Articles publicats en revistes (Patologia i Terapèutica Experimental)
Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL))

Citació

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. Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator. _eLife_. 2017. Vol. 6, núm. e23545. [consulta: 23 de gener de 2026]. ISSN: 2050-084X. [Disponible a: https://hdl.handle.net/2445/122570]

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