ArticleFASEB journal : official publication of the Federation of American Societies for Experimental Biology2011
Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses.
Article in FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
16 citing papers in PubMed, 24 citations in OpenAlex.
- Comparative analysis of ligand binding affinities and functional profiles at recombinant human β-adrenergic receptor subtypes 1, 2, and 3.The Journal of pharmacology and experimental therapeutics · 2026Review
- Comparing the Molecular Pharmacological Properties of Existing β-Blockers to Determine the Theoretically Most "Ideal" Anti-Cancer β-Blocker.Pharmacology research & perspectives · 2026Article
- Predicting compounds that interact with the 2 known agonist-induced conformations of the human β1-adrenoceptor.Molecular pharmacology · 2025Article
- Pancreatic Ductal Adenocarcinoma, β-blockers, and Antihistamines: A Clinical Trial Is Needed.Function (Oxford, England) · 2025Article
- Emerging Pharmacological and Invasive Therapies for Hypertrophic Cardiomyopathy with Obstructive Physiology.Cardiac failure review · 2025Review
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- Reply to: How carvedilol does not activate βNature communications · 2023Article
- Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine APharmacology research & perspectives · 2022Article
- Using Esterase Selectivity to Determine theACS pharmacology & translational science · 2020Article
- Novel selective βFASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2017Article
- Stimulation of βNaunyn-Schmiedeberg's archives of pharmacology · 2017Article
- Role of AKAP79/150 protein in β1-adrenergic receptor trafficking and signaling in mammalian cells.The Journal of biological chemistry · 2013Article
- β2-Adrenoceptor-mediated regulation of glucose uptake in skeletal muscle--ligand-directed signalling or a reflection of system complexity?Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- Cardiovascular responses to retigabine in conscious rats--under normotensive and hypertensive conditions.British journal of pharmacology · 2013Article
- Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.Journal of medicinal chemistry · 2013Article
- Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
β-Adrenoceptor antagonists differ in their degree of partial agonism. In vitro assays have provided information on ligand affinity, selectivity, and intrinsic efficacy. However, the extent to which these properties are manifest in vivo is less clear. Conscious freely moving rats, instrumented for measurement of heart rate (β1; HR) and hindquarters vascular conductance (β2; HVC) were used to measure receptor selectivity and ligand efficacy in vivo. CGP 20712A caused a dose-dependent decrease in basal HR (P<0.05, ANOVA) at 5 doses between 6.7 and 670 μg/kg (i.v.) and shifted the dose-response curve for isoprenaline to higher agonist concentrations without altering HVC responses. In contrast, at doses of 67 μg/kg (i.v.) and above, ICI 118551 substantially reduced the HVC response to isoprenaline without affecting HR responses. ZD 7114, xamoterol, and bucindolol significantly increased basal HR (ΔHR: +122 ± 12, + 129 ± 11, and + 59 ± 11 beats/min, respectively; n=6), whereas other β-blockers caused significant reductions (all at 2 mg/kg i.v.). The agonist effects of xamoterol and ZD 7114 were equivalent to that of the highest dose of isoprenaline. Bucindolol, however, significantly antagonized the response to the highest doses isoprenaline. An excellent correlation was obtained between in vivo and in vitro measures of β1-adrenoceptor efficacy (R(2)=0.93; P<0.0001).
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What OpenQuestion holds
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.