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A Photochromic Agonist for μ‐Opioid Receptors
Author(s) -
Schönberger Matthias,
Trauner Dirk
Publication year - 2014
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201309633
Subject(s) - g protein coupled receptor , photoswitch , rhodopsin , chemistry , receptor , neuroscience , azobenzene , agonist , opioid , biophysics , pharmacology , medicine , biochemistry , biology , retinal , photochemistry , organic chemistry , molecule
Opioid receptors (ORs) are widely distributed in the brain, the spinal cord, and the digestive tract and play an important role in nociception. All known ORs are G‐protein‐coupled receptors (GPCRs) of family A. Another well‐known member of this family, rhodopsin, is activated by light through the cis / trans isomerization of a covalently bound chromophore, retinal. We now show how an OR can be combined with a synthetic azobenzene photoswitch to gain light sensitivity. Our work extends the reach of photopharmacology and outlines a general strategy for converting Family A GPCRs, which account for the majority of drug targets, into photoreceptors.