Novel chalcone-based fluorescent human histamine H 3 receptor ligands as pharmacological tools

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. 
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 pK(i) value of 7.2). 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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Metadaten
Author:Miriam Tomasch, J. Stephan Schwed, Lilia Weizel, Holger Stark
URN:urn:nbn:de:hebis:30:3-275995
DOI:http://dx.doi.org/10.3389/fnsys.2012.00014
ISSN:1662-5137
Pubmed Id:http://www.ncbi.nlm.nih.gov/pubmed?term=22470321
Parent Title (English):Frontiers in systems neuroscience
Publisher:Frontiers Research Foundation
Place of publication:Lausanne
Document Type:Article
Language:English
Date of Publication (online):2012/11/16
Date of first Publication:2012/03/26
Publishing Institution:Univ.-Bibliothek Frankfurt am Main
Release Date:2012/11/16
Tag:fluorescence confocal laser scanning microscopy; fluorescent ligand; human histamine H3 receptor; pharmacological tool
Volume:6
Issue:Article 14
Pagenumber:16
Note:
Copyright: © 2012 Tomasch, Schwed, Weizel and Stark. This is an open-access article distributed under the terms of the Creative Commons Attribution Non Commercial License, which permits non-commercial use, distribution, and reproduction in other forums, provided the original authors and source are credited.
HeBIS PPN:318582643
Institutes:Pharmazie
Zentrum für Arzneimittelforschung, Entwicklung und Sicherheit
Dewey Decimal Classification:610 Medizin und Gesundheit
Sammlungen:Universitätspublikationen
Licence (German):License LogoCreative Commons - Namensnennung-Nicht kommerziell 3.0

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