TY  - JOUR
A1  - Tomasch, Miriam
A1  - Schwed, J. Stephan
A1  - Weizel, Lilia
A1  - Stark, Holger
T1  - Novel chalcone-based fluorescent human histamine H 3 receptor ligands as pharmacological tools
T2  - Frontiers in systems neuroscience
N2  - 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.
KW  - human histamine H3 receptor
KW  - fluorescent ligand
KW  - fluorescence confocal laser scanning microscopy
KW  - pharmacological tool
Y1  - 2012
UR  - http://publikationen.ub.uni-frankfurt.de/frontdoor/index/index/docId/27599
UR  - https://nbn-resolving.org/urn:nbn:de:hebis:30:3-275995
SN  - 1662-5137
N1  - 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.
VL  - 6
IS  - Article 14
PB  - Frontiers Research Foundation
CY  - Lausanne
ER  -