1. High-affinity fluorescent ligands for the 5-HT3 receptor
- Author
-
Sarah C. R. Lummis, Sanjeev Kumar V. Vernekar, Jonathan Simonin, J. Daniel Hothersall, Christopher N. Connolly, Martin Lochner, and Andrew J. Thompson
- Subjects
Models, Molecular ,Clinical Biochemistry ,Pharmaceutical Science ,Crystallography, X-Ray ,Ligands ,Biochemistry ,0302 clinical medicine ,Radioligand binding ,Drug Discovery ,Chlorocebus aethiops ,Receptor ,GFP, green fluorescent protein ,0303 health sciences ,biology ,Molecular Structure ,Chemistry ,musculoskeletal, neural, and ocular physiology ,nACh, nicotinic acetylcholine ,Stereoisomerism ,Fluorescence ,3. Good health ,5-HT3 receptor ,In vivo imaging ,COS Cells ,Molecular Medicine ,FITC, fluorescein isothiocyanate ,GABAA, γ-aminobutyric acid type A ,Stereochemistry ,Fluorescent ligands ,SAR, Structure–activity relationship ,5-HT3R, 5-HT3 receptor ,Article ,Small Molecule Libraries ,03 medical and health sciences ,Structure-Activity Relationship ,Structure–activity relationship ,Molecule ,Animals ,Humans ,Molecular Biology ,030304 developmental biology ,ComputingMethodologies_COMPUTERGRAPHICS ,PEG, polyethylene glycol ,Fluorescent Dyes ,Dose-Response Relationship, Drug ,Organic Chemistry ,Cys-loop ligand-gated ion channels ,nervous system ,biology.protein ,Receptors, Serotonin, 5-HT3 ,030217 neurology & neurosurgery ,BODIPY, 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene ,Conjugate - Abstract
Graphical abstract, The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT3AR.
- Published
- 2012