ArticleNaunyn-Schmiedeberg's archives of pharmacology2006
Comparison of three radioligands for the labelling of human beta-adrenoceptor subtypes.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 52 citations in OpenAlex.
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- Hypoxia-Dependent Upregulation of VEGF Relies on β3-Adrenoceptor Signaling in Human Retinal Endothelial and Müller Cells.International journal of molecular sciences · 2025Article
- Age-dependent effects of the βPflugers Archiv : European journal of physiology · 2024Article
- Adrenoceptor Expression and Function in the Endocrine Pancreas.Handbook of experimental pharmacology · 2024Review
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- Cardiac βBritish journal of pharmacology · 2019Review
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- Agonist-induced desensitisation of βBritish journal of pharmacology · 2019Review
- Everything You Always Wanted to Know about βCells · 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
- Rat β₃-adrenoceptor protein expression: antibody validation and distribution in rat gastrointestinal and urogenital tissues.Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
- Functional involvement of β3-adrenergic receptors in melanoma growth and vascularization.Journal of molecular medicine (Berlin, Germany) · 2013Article
- Agonist-induced desensitization of human β3-adrenoceptors expressed in human embryonic kidney cells.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- Pharmacological profile of β3-adrenoceptor agonists in clinical development for the treatment of overactive bladder syndrome.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- The β-blocker Nebivolol Is a GRK/β-arrestin biased agonist.PloS one · 2013Article
- Specificity evaluation of antibodies against human β3-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2012Article
- Functional investigation of β-adrenoceptors in human isolated detrusor focusing on the novel selective β3-adrenoceptor agonist KUC-7322.Naunyn-Schmiedeberg's archives of pharmacology · 2012Article
- Beta3-adrenoreceptor stimulation ameliorates myocardial ischemia-reperfusion injury via endothelial nitric oxide synthase and neuronal nitric oxide synthase activation.Journal of the American College of Cardiology · 2011Article
- More severe cellular phenotype in human idiopathic dilated cardiomyopathy compared to ischemic heart disease.Journal of muscle research and cell motility · 2010Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have compared the ability of three radioligands, [(125)I]-cyanopindolol, [(3)H]-CGP 12,177 and [(3)H]-dihydroalprenolol, to label the three human beta-adrenoceptor subtypes. Saturation and competition binding experiments were performed using membrane preparations from Chinese hamster ovary cells stably transfected with the three subtypes. While [(3)H]-CGP 12,177 had very similar affinity for beta(1)- and beta(2)-adrenoceptors (about 40 pM), [(125)I]-cyanopindolol and [(3)H]-dihydroalprenolol had 4- to 6-fold higher affinity for beta(2)- as compared to beta(1)-adrenoceptors (10 vs 45 and 187 vs 1,021 pM, respectively). The affinity of [(125)I]-cyanopindolol at beta(3)-adrenoceptors was considerably lower (440 pM) than at the other two subtypes. The beta(3)-adrenoceptor affinity of [(3)H]-CGP 12,177 and [(3)H]-dihydroalprenolol was so low that it could not be estimated within the tested range of radioligand concentrations (up to 4,000 pM and 30,000 pM for [(3)H]-CGP 12,177 and [(3)H]-dihydroalprenolol, respectively). We conclude that all three radioligands are ill-suited to label beta(3)-adrenoceptors, particularly in preparations co-expressing multiple subtypes. In the absence of alternatives, [(125)I]-cyanopindolol appears the least unsuitable to label beta(3)-adrenoceptors. There is a need for high-affinity radioligands which are either selective for beta(3)-adrenoceptors or reasonably non-selective among all three beta-adrenoceptor subtypes.
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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.