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A novel G protein‐biased agonist at the μ opioid receptor induces substantial receptor desensitisation through G protein‐coupled receptor kinase
Author(s) -
Groom Sam,
Blum Nina K.,
Conibear Alexandra E.,
Disney Alexander,
Hill Rob,
Husbands Stephen M.,
Li Yangmei,
Toll Lawrence,
Kliewer Andrea,
Schulz Stefan,
Henderson Graeme,
Kelly Eamonn,
Bailey Chris P.
Publication year - 2023
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.15334
Subject(s) - agonist , g protein coupled receptor , g protein coupled receptor kinase , functional selectivity , receptor , g protein , opioid receptor , microbiology and biotechnology , protein kinase c , chemistry , protein kinase a , intrinsic activity , arrestin , pharmacology , biology , signal transduction , biochemistry , kinase
G protein-biased μ opioid receptor agonists have the potential to induce less receptor desensitisation and tolerance than balanced opioids. Here, we investigated if the cyclic endomorphin analogue Tyr-c[D-Lys-Phe-Tyr-Gly] (Compound 1) is a G protein-biased μ agonist and characterised its ability to induce rapid receptor desensitisation in mammalian neurones.