- Fluorescent human EP3 receptor antagonists
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Exchange of the lipophilc part of ortho-substituted cinnamic acid lead structures with different small molecule fluorophoric moieties via a dimethylene spacer resulted in hEP3R ligands with affinities in the nanomolar concentration range. Synthesized compounds emit fluorescence in the blue, green, and red range of light and have been tested concerning their potential as a pharmacological tool. hEP3Rs were visualized by confocal laser scanning microscopy on HT-29 cells, on murine kidney tissues, and on human brain tissues and functionally were characterized as antagonists on human platelets. Inhibition of PGE2 and collagen-induced platelet aggregation was measured after preincubation with novel hEP3R ligands. The pyryllium-labeled ligand 8 has been shown as one of the most promising structures, displaying a useful fluorescence and highly affine hEP3R antagonists.
- Tomasch, Miriam,Schwed, J. Stephan,Kuczka, Karina,Meyer Dos Santos, Sascha,Harder, Sebastian,Nuesing, Rolf M.,Paulke, Alexander,Stark, Holger
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supporting information
p. 774 - 779
(2012/11/13)
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- Method for locating hidden microorganism contaminated surfaces in industrial water systems
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A method for locating hidden microorganism contaminated surfaces in industrial water systems is described and claimed. The method works by applying a solution or dispersion of a fluorogenic reagent in water to the hidden water contact surfaces of said industrial water system and allowing said fluorogenic reagent to react with any hidden microorganisms present, wherein said fluorogenic reagent is selected from the group of fluorogenic reagents that are known to react with microorganisms such that a fluorescent signal of said fluorogenic reagent is detectable in such a way as to make the detection of the fluorescent signal indicate that there are hidden microorganisms present on the water contact surfaces of the equipment and piping.
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