ArticleACS medicinal chemistry letters2013
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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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.
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Who cites it
8 citing papers in PubMed, 25 citations in OpenAlex.
- Recent Progress of Fluorescence Sensors for Histamine in Foods.Biosensors · 2022Review
- New Chemical Biology Tools for the Histamine Receptor Family.Current topics in behavioral neurosciences · 2022Article
- Chemical Probes for Histamine Receptor Subtypes.Current topics in behavioral neurosciences · 2022Article
- The Histamine H3 Receptor Antagonist E159 Reverses Memory Deficits Induced by Dizocilpine in Passive Avoidance and Novel Object Recognition Paradigm in Rats.Frontiers in pharmacology · 2017Article
- Pharmacological Characterization of Human Histamine Receptors and Histamine Receptor Mutants in the Sf9 Cell Expression System.Handbook of experimental pharmacology · 2017Review
- Non-imidazole-based histamine H3 receptor antagonists with anticonvulsant activity in different seizure models in male adult rats.Drug design, development and therapy · 2016Article
- The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs.British journal of pharmacology · 2014Review
- Drug-likeness approach of 2-aminopyrimidines as histamine H3 receptor ligands.Drug design, development and therapy · 2014Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A piperidine-based lead structure for the human histamine H3 receptor (hH3R) was coupled with the BODIPY fluorophore and resulted in a strong green fluorescent (quantum yield, 0.92) hH3R ligand with affinity in the nanomolar concentration range (K i hH3R = 6.51 ± 3.31 nM), named Bodilisant. Screening for affinities at histamine and dopamine receptor subtypes showed high hH3R preference. Bodilisant was used for visualization of hH3R in hH3R overexpressing HEK-293 cells with fluorescence confocal laser scanning microscopy. In addition, in native human brain tissues, Bodilisant showed clear and displaceable images of labeled hH3R.
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Registered trials
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