ArticleThe Journal of clinical investigation2007
Real-time optical recording of beta1-adrenergic receptor activation reveals supersensitivity of the Arg389 variant to carvedilol.
Article in The Journal of clinical investigation, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 63 papers, 2 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
63 citing papers in PubMed, 2 syntheses or guidelines pooled it, 136 citations in OpenAlex.
- Pooled it
- Association of hypertension drug target genes with blood pressure and hypertension in 86,588 individuals.Hypertension (Dallas, Tex. : 1979) · 2011Pooled it
- Decoupling between activation time and steady-state level in input-output responses.PLoS computational biology · 2026Article
- Light-Based Molecular Tools to Precisely Monitor and Operate β-Adrenoceptors.Medicinal research reviews · 2026Review
- Decoupling between activation time and steady-state level in input-output responses.bioRxiv : the preprint server for biology · 2025Article
- The potential role of carvedilol in COVID-19 management: perspective and take-away.Inflammopharmacology · 2025Review
- Altered O-glycosylation of βThe FEBS journal · 2025Article
- Exploiting Cell-Based Assays to Accelerate Drug Development for G Protein-Coupled Receptors.International journal of molecular sciences · 2024Review
- Genetic Variants of Adrenoceptors.Handbook of experimental pharmacology · 2024Review
- Two-step structural changes in M3 muscarinic receptor activation rely on the coupled GNature communications · 2023Article
- Investigating G-protein coupled receptor signalling with light-emitting biosensors.Frontiers in physiology · 2023Review
- Genetically encoded tools for in vivo G-protein-coupled receptor agonist detection at cellular resolution.Clinical and translational medicine · 2022Review
- Genetically encoded fluorescent biosensors for GPCR research.Frontiers in cell and developmental biology · 2022Review
- Adrenergic receptors gene polymorphisms and autonomic nervous control of heart and vascular tone.Physiological research · 2021Review
- Neurohormonal modulation in pulmonary arterial hypertension.The European respiratory journal · 2021Review
- Multiple GPCR Functional Assays Based on Resonance Energy Transfer Sensors.Frontiers in cell and developmental biology · 2021Review
- Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4.Molecular pharmacology · 2020Article
- A high-resolution description of βNature communications · 2020Article
- Optical approaches for single-cell and subcellular analysis of GPCR-G protein signaling.Analytical and bioanalytical chemistry · 2019Review
- GαNature communications · 2017Article
3 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
Abstract
Antagonists of beta-adrenergic receptors (beta-ARs) have become a main therapeutic regimen for the treatment of heart failure even though the mechanisms of their beneficial effects are still poorly understood. Here, we used fluorescent resonance energy transfer-based (FRET-based) approaches to directly monitor activation of the beta(1)-AR and downstream signaling. While the commonly used beta-AR antagonists metoprolol, bisoprolol, and carvedilol displayed varying degrees of inverse agonism on the Gly389 variant of the receptor (i.e., actively switching off the beta(1)-AR), surprisingly, only carvedilol showed very specific and marked inverse agonist effects on the more frequent Arg389 variant. These specific effects of carvedilol on the Arg389 variant of the beta(1)-AR were also seen for control of beating frequency in rat cardiac myocytes expressing the 2 receptor variants. This FRET sensor permitted direct observation of activation of the beta(1)-AR in living cells in real time. It revealed that beta(1)-AR variants dramatically differ in their responses to diverse beta blockers, with possible consequences for their clinical use.
Indexed as
Identifiers
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.