ArticleJournal of medicinal chemistry2011
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Using a NanoBRET-Based Ligand-Binding Assay at the βPharmacology research & perspectives · 2026Article
- A BBB-permeable βScience advances · 2026Article
- Light-Based Molecular Tools to Precisely Monitor and Operate β-Adrenoceptors.Medicinal research reviews · 2026Review
- Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine HJournal of medicinal chemistry · 2022Article
- Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2-adrenoceptor in CRISPR/Cas9 genome-edited HEK293T cells at low expression levels.Pharmacology research & perspectives · 2021Article
- Fluorescent HACS medicinal chemistry letters · 2020Article
- Article
- Visualizing Ligand Binding to a GPCR In Vivo Using NanoBRET.iScience · 2018Article
- Micro-pharmacokinetics: Quantifying local drug concentration at live cell membranes.Scientific reports · 2018Article
- High-Affinity Functional Fluorescent Ligands for Human β-Adrenoceptors.Scientific reports · 2017Article
- PyrrolylBODIPYs: Syntheses, Properties, and Application as Environment-Sensitive Fluorescence Probes.ACS omega · 2017Article
- Impact of salt stress, cell death, and autophagy on peroxisomes: quantitative and morphological analyses using small fluorescent probe N-BODIPY.Scientific reports · 2017Article
- Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the humanPharmacology research & perspectives · 2016Article
- Fluorescence- and bioluminescence-based approaches to study GPCR ligand binding.British journal of pharmacology · 2016Review
- Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.ACS medicinal chemistry letters · 2015Article
- Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2014Article
- The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs.British journal of pharmacology · 2014Review
- Biophysical Detection of Diversity and Bias in GPCR Function.Frontiers in endocrinology · 2014Review
- Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.Biochimica et biophysica acta · 2014Review
- Synthesis of BODIPY derivatives substituted with various bioconjugatable linker groups: a construction kit for fluorescent labeling of receptor ligands.Journal of fluorescence · 2014Article
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Authors and funding
7 authors.
Funding
Abstract
The growing practice of exploiting noninvasive fluorescence-based techniques to study G protein-coupled receptor pharmacology at the single cell and single molecule level demands the availability of high-quality fluorescent ligands. To this end, this study evaluated a new series of red-emitting ligands for the human β-adrenoceptor family. Upon the basis of the orthosteric ligands propranolol, alprenolol, and pindolol, the synthesized linker-modified congeners were coupled to the commercially available fluorophore BODIPY 630/650-X. This yielded high-affinity β-adrenoceptor fluorescent ligands for both the propranolol and alprenolol derivatives; however, the pindolol-based products displayed lower affinity. A fluorescent diethylene glycol linked propranolol derivative (18a) had the highest affinity (log K(D) of -9.53 and -8.46 as an antagonist of functional β2- and β1-mediated responses, respectively). Imaging studies with this compound further confirmed that it can be employed to selectively label the human β2-adrenoceptor in single living cells, with receptor-associated binding prevented by preincubation with the nonfluorescent β2-selective antagonist 3-(isopropylamino)-1-[(7-methyl-4-indanyl)oxy]butan-2-ol (ICI 118551) ( J. Cardiovasc. Pharmacol.1983, 5, 430-437. ).
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