Agonist-induced desensitisation of β3 -adrenoceptors: Where, when, and how?

British Journal of Pharmacology
Katerina OkekeMartin C Michel

Abstract

β3 -Adrenoceptor agonists have proven useful in the treatment of overactive bladder syndrome, but it is not known whether their efficacy during chronic administration may be limited by receptor-induced desensitisation. Whereas the β2 -adrenoceptor has phosphorylation sites that are important for desensitisation, the β3 -adrenoceptor lacks these; therefore, it had been assumed that β3 -adrenoceptors are largely resistant to agonist-induced desensitisation. While all direct comparative studies demonstrate that β3 -adrenoceptors are less susceptible to desensitisation than β2 -adrenoceptors, desensitisation of β3 -adrenoceptors has been observed in many models and treatment settings. Chimeric β2 - and β3 -adrenoceptors have demonstrated that the C-terminal tail of the receptor plays an important role in the relative resistance to desensitisation but is not the only relevant factor. While the evidence from some models, such as transfected CHO cells, is inconsistent, it appears that desensitisation is observed more often after long-term (hours to days) than short-term (minutes to hours) agonist exposure. When it occurs, desensitisation of β3 -adrenoceptors can involve multiple levels including down-regulation of its mRNA and the rec...Continue Reading

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Citations

Feb 10, 2020·International Journal of Urology : Official Journal of the Japanese Urological Association·Martin C Michel
Mar 15, 2019·British Journal of Pharmacology·Yasuhiko IgawaMartin C Michel
Jun 27, 2019·British Journal of Pharmacology·Martin C MichelRoger J Summers
Dec 20, 2019·Naunyn-Schmiedeberg's Archives of Pharmacology·Massimo Dal MonteMartin C Michel
Apr 19, 2019·Cells·Giorgia Schena, Michael J Caplan
Dec 2, 2020·Cells·Betul R ErdoganEbru Arioglu-Inan
Jan 2, 2021·Cellular Signalling·Michael Ippolito, Jeffrey L Benovic
Dec 6, 2020·Cells·Lauriane Y M MichelJean-Luc Balligand
Jan 29, 2021·British Journal of Pharmacology·Samantha L SaundersTimothy V Murphy
Dec 1, 2021·The Journal of Clinical Investigation·Joseph M ValentineAlan R Saltiel

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