Illuminating Phenylazopyridines To Photoswitch Metabotropic Glutamate Receptors: From the Flask to the Animals

Overview

Journal ACS Cent Sci

Specialty Chemistry

Date 2017 Feb 3

PMID 28149957

Citations 22

Authors

Xavier Gomez-Santacana

Silvia Pittolo

Xavier Rovira

Marc Lopez

Charleine Zussy

James A R Dalton

Adele Faucherre

Chris Jopling

Jean-Philippe Pin

Francisco Ciruela

Cyril Goudet

Jesus Giraldo

Pau Gorostiza

Amadeu Llebaria

Affiliations

Soon will be listed here.

Abstract

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 (mGlu). Here we describe the factors needed to achieve an operational molecular photoisomerization and its effective translation into and 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 and . 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.

Citing Articles

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