ArticleNaunyn-Schmiedeberg's archives of pharmacology2014
Do β-adrenoceptor agonists induce homologous or heterologous desensitization in rat urinary bladder?
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 30 citations in OpenAlex.
- Unveiling the bladder's early response to acute glucosuria: first evidence from an animal study.International urology and nephrology · 2025Article
- βNeurourology and urodynamics · 2025Review
- Vibegron shows high selectivity and potent agonist activity for β3-adrenoceptors, irrespective of receptor density.PloS one · 2023Article
- Upregulation of βNaunyn-Schmiedeberg's archives of pharmacology · 2020Review
- Normalization of organ bath contraction data for tissue specimen size: does one approach fit all?Naunyn-Schmiedeberg's archives of pharmacology · 2020Article
- Agonist-induced desensitisation of βBritish journal of pharmacology · 2019Review
- βBritish journal of pharmacology · 2019Review
- Desensitization of cAMP Accumulation via Human β3-Adrenoceptors Expressed in Human Embryonic Kidney Cells by Full, Partial, and Biased Agonists.Frontiers in pharmacology · 2019Article
- Urinary Bladder Weight and Function in a Rat Model of Mild Hyperglycemia and Its Treatment With Dapagliflozin.Frontiers in pharmacology · 2019Article
- Mirabegron relaxes urethral smooth muscle by a dual mechanism involving β3 -adrenoceptor activation and α1 -adrenoceptor blockade.British journal of pharmacology · 2016Article
- Contractile function of smooth muscle retained after overnight storage.Naunyn-Schmiedeberg's archives of pharmacology · 2015Article
- Are blood vessels a target to treat lower urinary tract dysfunction?Naunyn-Schmiedeberg's archives of pharmacology · 2015Article
- β3-Adrenoceptor-mediated relaxation of rat and human urinary bladder: roles of BKCa channels and Rho kinase.Naunyn-Schmiedeberg's archives of pharmacology · 2015Article
- Rat β₃-adrenoceptor protein expression: antibody validation and distribution in rat gastrointestinal and urogenital tissues.Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
- How significant are your data? The need for a culture shift.Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
- The pharmacological rationale for combining muscarinic receptor antagonists and β-adrenoceptor agonists in the treatment of airway and bladder disease.Current opinion in pharmacology · 2014Review
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Authors and funding
1 author at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
β3-Adrenoceptor agonists have recently been introduced for the symptomatic treatment of the overactive bladder syndrome. As such treatment is not curative, long-term treatment is anticipated to be required. As the susceptibility of β3-adrenoceptors to undergo agonist-induced desensitization is cell type- and tissue-dependent, we have explored whether pre-treatment with a β-adrenoceptor agonist will attenuate subsequent relaxation responses to freshly added agonist using rat urinary bladder as a model. We have used the prototypical β-adrenoceptor agonist isoprenaline, the β2-selective fenoterol and the β3-selective CL 316,243 and mirabegron as well as the receptor-independent bladder relaxant forskolin. We show that a 6-h pre-treatment with agonist can significantly reduce subsequent relaxation against KCl-induced smooth muscle tone, but agonist-induced desensitization was also observed with longer pre-treatments or against passive tension. The agonist-induced desensitization was prominent for the β2 component of rat bladder relaxation but much weaker or even absent for the β3 component. Moreover, β-adrenoceptor agonist pre-treatment reduced contractile responses to the muscarinic agonist carbachol and the receptor-independent stimulus KCl. Taken together these data do not support the hypothesis that the long-term clinical efficacy of β3-adrenoceptor agonists in the treatment of the overactive bladder syndrome will be limited by receptor desensitization. Rather they raise the possibility that such treatment may not only cause smooth muscle relaxation but also may attenuate hyper-contractility of the bladder.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.