Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities.
Omega-piperidinoalkanamine derivatives with fluorescent moieties (2-cyanoisoindol-1-yl, 7-nitrobenzofurazan-4-yl) have been synthesized starting from piperidine in three steps. The compounds display moderate to good histamine hH(3) receptor affinities with K(i) values ranging from 178 to 11nM. The new compounds may act as tools for identification and understanding of the binding site on the histamine H(3) receptor.
Amon
Michael
M
Johann Wolfgang Goethe-Universität, ZAFES, Biozentrum, Institut für Pharmazeutische Chemie, 60431 Frankfurt, Germany.
Ligneau
Xavier
X
Schwartz
Jean-Charles
JC
Stark
Holger
H
D005456:Fluorescent Dyes / Q000378:metabolism*; D008024:Ligands; D036103:Nanotechnology; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013050:Spectrometry, Fluorescence
D005456:Fluorescent Dyes; D008024:Ligands; D018100:Receptors, Histamine H3