title: Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities.
abstract: 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.
authors.affiliation: Johann Wolfgang Goethe-Universität, ZAFES, Biozentrum, Institut für Pharmazeutische Chemie, 60431 Frankfurt, Germany.
authors.forename: Michael
authors.initials: M
authors.lastname: Amon
authors.forename: Xavier
authors.initials: X
authors.lastname: Ligneau
authors.forename: Jean-Charles
authors.initials: JC
authors.lastname: Schwartz
authors.forename: Holger
authors.initials: H
authors.lastname: Stark
mesh_terms: D005456:Fluorescent Dyes / Q000378:metabolism*; D008024:Ligands; D036103:Nanotechnology; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013050:Spectrometry, Fluorescence
chemical_list: D005456:Fluorescent Dyes; D008024:Ligands; D018100:Receptors, Histamine H3