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Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities
Michael Amon1, Xavier Ligneau, Jean-Charles Schwartz
1Johann Wolfgang Goethe-Universität, ZAFES, Biozentrum, Institut für Pharmazeutische Chemie, 60431 Frankfurt, Germany.
Bioorganic & Medicinal Chemistry Letters
|January 26, 2006
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.
