Journal
FRONTIERS IN SYSTEMS NEUROSCIENCE
Volume 6, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fnsys.2012.00014
Keywords
human histamine H-3 receptor; fluorescent ligand; fluorescence confocal laser scanning microscopy; pharmacological tool
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Funding
- Hesse LOEWE Schwerpunkte NeFF
- OSP
- AFA
- 14'7 EU COST Actions [BM0806, BM1007, CM1103]
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Novel fluorescent chalcone-based ligands at human histamine H-3 receptors (hH(3)R) have been designed, synthesized, and characterized. Compounds described are non-imidazole analogs of ciproxifan with a tetralone motif. Tetralones as chemical precursors and related fluorescent chalcones exhibit affinities at hH(3)R in the same concentration range like the reference antagonist ciproxifan (hH(3)R pKi value of 72). Fluorescence characterization of our novel ligands shows emission maxima about 570 nm for yellow fluorescent chalcones and >600 nm for the red fluorescent derivatives. Interferences to cellular autofluorescence could be excluded. All synthesized chalcone compounds could be used to visualize hH(3)R proteins in stably transfected HEK-293 cells using confocal laser scanning fluorescence microscopy. These novel fluorescent ligands possess high potential to be used as pharmacological tools for hH(3)R visualization in different tissues.
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