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Title: Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
Author: 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
Keywords: Neurociències
Ratolins (Animals de laboratori)
Tractament del dolor
Mice (Laboratory animals)
Pain treatment
Issue Date: 11-Apr-2017
Publisher: eLife Sciences
Abstract: 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.
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It is part of: eLife, 2017, vol. 6, p. e23545
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ISSN: 2050-084X
Appears in Collections:Articles publicats en revistes (Patologia i Terapèutica Experimental)
Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL))

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