A novel G protein‐biased agonist at the μ opioid receptor induces substantial receptor desensitisation through G protein‐coupled receptor kinase | Zendy

Groom Sam | Zendy; Blum Nina K. | Zendy; Conibear Alexandra E. | Zendy; Disney Alexander | Zendy; Hill Rob | Zendy; Husbands Stephen M. | Zendy; Li Yangmei | Zendy; Toll Lawrence | Zendy; Kliewer Andrea | Zendy; Schulz Stefan | Zendy; Henderson Graeme | Zendy; Kelly Eamonn | Zendy; Bailey Chris P. | Zendy

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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) - g protein coupled receptor kinase , 5 ht5a receptor , agonist , enzyme linked receptor , opioid receptor , g protein coupled receptor , receptor , chemistry , tropomyosin receptor kinase b , functional selectivity , pharmacology , tropomyosin receptor kinase c , microbiology and biotechnology , neuroscience , medicine , biology , biochemistry , platelet derived growth factor receptor , growth factor , neurotrophic factors

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.

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