ArticleNaunyn-Schmiedeberg's archives of pharmacology2013
In vitro and in vivo pharmacological profile of the selective β3-adrenoceptor agonist mirabegron in rats.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 46 citations in OpenAlex.
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- Mirabegron, a Selective β3-Adrenergic Receptor Agonist, as a Potential Anti-Obesity Drug.Journal of clinical medicine · 2023Review
- Selectivity and Maximum Response of Vibegron and Mirabegron for βCurrent therapeutic research, clinical and experimental · 2022Article
- Concentration-dependent alphaFrontiers in pharmacology · 2021Article
- Mirabegron: potential off target effects and uses beyond the bladder.British journal of pharmacology · 2018Review
- The efficacy of mirabegron in the treatment of urgency and the potential utility of combination therapy.Therapeutic advances in urology · 2018Review
- On the Site and Mechanism of Action of βInternational neurourology journal · 2017Review
- The link between vascular dysfunction, bladder ischemia, and aging bladder dysfunction.Therapeutic advances in urology · 2017Review
- Mirabegron relaxes urethral smooth muscle by a dual mechanism involving β3 -adrenoceptor activation and α1 -adrenoceptor blockade.British journal of pharmacology · 2016Article
- Drug therapy of overactive bladder--what is coming next?Korean journal of urology · 2015Review
- Prostaglandin E2 excitatory effects on rat urinary bladder: a comparison between the β-adrenoceptor modulation of non-voiding activity in vivo and micro-contractile activity in vitro.Naunyn-Schmiedeberg's archives of pharmacology · 2015Article
- Beta adrenergic modulation of spontaneous microcontractions and electrical field-stimulated contractions in isolated strips of rat urinary bladder from normal animals and animals with partial bladder outflow obstruction.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
- Do β-adrenoceptor agonists induce homologous or heterologous desensitization in rat urinary bladder?Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
- Pharmacological profile of the selective β3-adrenoceptor agonist mirabegron in cynomolgus monkeys.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- β3-receptor agonists for overactive bladder--new frontier or more of the same?Current urology reports · 2013Review
- Pharmacological profile of β3-adrenoceptor agonists in clinical development for the treatment of overactive bladder syndrome.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- New developments in the management of overactive bladder: focus on mirabegron and onabotulinumtoxinA.Therapeutics and clinical risk management · 2013Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
To investigate the pharmacological properties of mirabegron in in vitro and in vivo, the effects on cAMP accumulation in Chinese hamster ovary (CHO) cells expressing rat β-adrenoceptors, the relaxant activity in isolated rat bladder smooth muscle, and the voiding effects in cerebral infarcted rats were evaluated. Mirabegron increased cAMP accumulation with EC(50) value and intrinsic activity of 19 nmol/L and 1.0, respectively, in CHO cells expressing rat β(3)-adrenoceptors. The EC(50) values and the intrinsic activities of mirabegron were 610 nmol/L and 0.6 for rat β(1)-adrenoceptors and were sumless and 0.1 for β(2)-adrenoceptors, respectively. Mirabegron showed concentration-dependent relaxant and full agonistic effects in rat bladder strips under passive tension with EC(50) value of 290 nmol/L. The concentration-response curve of mirabegron was affected neither by the β(1)-adrenoceptor selective antagonist CGP-20712A nor by the β(2)-adrenoceptor selective antagonist ICI-118,551. In in vivo studies with cerebral infarcted rats, a significant decrease in the volume voided per micturition compared with sham-operated rats was observed. Mirabegron dose-dependently increased the volume voided per micturition. In conclusion, we have extended the selectivity profile of mirabegron to rats and demonstrated that it is effective via stimulation of β(3)-adrenoceptors in a rat cerebral infarction model of detrusor overactivity.
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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.