A novel G protein-biased agonist at the μ opioid receptor induces substantial receptor desensitization through G protein-coupled receptor kinase

Autor: Nina K Blum, Alexandra E. Conibear, Lawrence Toll, Christopher P Bailey, Sam Groom, Stefan Schulz, Andrea Kliewer, Yangmei Li, Robert J. Hill, Graeme Henderson, Stephen M. Husbands, Alexander Disney, Eamonn Kelly

Publikováno v: Groom, S, Blum, N K, Conibear, A E, Disney, A, Hill, R, Husbands, S M, Li, Y, Toll, L, Kliewer, A, Schulz, S, Henderson, G, Kelly, E & Bailey, C P 2020, ' A novel G protein-biased agonist at the μ opioid receptor induces substantial receptor desensitization through G protein-coupled receptor kinase ', British Journal of Pharmacology . https://doi.org/10.1111/bph.15334

Background and purpose 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] (Com

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https://purehost.bath.ac.uk/ws/files/214871251/Groom_et_al_Accepted_version_inc_figures.pdf