期刊
ACS CENTRAL SCIENCE
卷 3, 期 1, 页码 81-91出版社
AMER CHEMICAL SOC
DOI: 10.1021/acscentsci.6b00353
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资金
- RecerCaixa foundation [2010ACUP00378]
- Marato de TV3 Foundation [110230, 110231, 110232, 111531]
- Catalan government [2010 BP-A 00194, 2012FI_B 01122, 2012 CTP 00033, 2012 BE1 00597, 2014SGR-1251, 2014SGR-00109]
- Spanish Government [CTQ2014-57020-R, PCIN-2013-017-C03-01, PIE14/00034, SAF2014-55700-P, PCIN-2013-019-C03-03, SAF2014-58396-R]
- AWT [SBO-140028]
- ERANET Neuron LIGHTPAIN project
- SynBio MODU-LIGHTOR
- Human Brain Project WAVESCALES
- Ramon Areces foundation
- Agence Nationale de la Recherche [ANR-16-CE16-0010]
- ICREA Funding Source: Custom
Phenylazopyridines are photoisomerizable compounds with high potential to control biological functions with light. We have obtained a series of phenylazopyridines with light dependent activity as negative allosteric modulators (NAM) of metabotropic glutamate receptor subtype 5 (mGlu5). Here we describe the factors needed to achieve an operational molecular photoisomerization and its effective translation into in vitro and in vivo receptor photoswitching, which includes zebrafish larva motility and the regulation of the antinociceptive effects in mice. The combination of light and some specific phenylazopyridine ligands displays atypical pharmacological profiles, including light-dependent receptor overactivation, which can be observed both in vitro and in vivo. Remarkably, the localized administration of light and a photoswitchable compound in the peripheral tissues of rodents or in the brain amygdalae results in an illumination-dependent analgesic effect. The results reveal a robust translation of the phenylazopyridine photoisomerization to a precise photoregulation of biological activity.
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