期刊
ELIFE
卷 6, 期 -, 页码 -出版社
ELIFE SCIENCES PUBLICATIONS LTD
DOI: 10.7554/eLife.23545
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资金
- Ministerio de Economia y Competitividad [PCIN-2013-018-C03-02, SAF2014-58396-R, CTQ2013-48767-C3-1-R, CTQ2015-71896-REDT, PCIN-2013-017-C03-01, CTQ2014-57020-R, SAF2014-55700-P, PCIN-2013-019-C03-03]
- Fondation pour la Recherche Medicale [DEQ20130326522]
- European Commission [Neuron eranet, ANR-12-NEUR-0003-05]
- Agence Nationale de la Recherche [ANR-12-NEUR-0003]
- Generalitat de Catalunya [2014SGR304, 2014SGR109, 2014CTP0002, 2014 SGR 1054]
- Ministero della Salute ERA-NET NEURON LIGHTGLUPAIN
- Institute de Salud Carlos III [PIE14/00034]
- Fundacio la Marato de TV3 [20152031]
- Institucio Catalana de Recerca i Estudis Avangats [ICREA Academia-2010]
- Agentschap voor Innovatie door Wetenschap en Technologie [SBO-140028]
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 (mGlu(5)) 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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