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G‐Protein‐Coupled Receptors: Sustained Signaling via Intracellular Megaplexes and Pathway‐Specific Drugs
Author(s) -
Link Andreas,
Müller Christa E.
Publication year - 2016
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.201609015
Subject(s) - receptor , agonist , pharmacology , chemistry , opioid , g protein coupled receptor , addiction , analgesic , hypoventilation , intracellular , medicine , neuroscience , respiratory system , biology , biochemistry
Together forever? Functional selection was applied to finally achieve separation of the analgesic properties of opiods from serious side effects such as potentially lethal respiratory depression. A Gi‐biased μ‐opioid‐receptor agonist (PZM21) was identified that stabilizes previously unexplored receptor conformations. This compound relieves pain in mice without causing hypoventilation or addiction.