Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1938-40. doi: 10.1016/j.bmcl.2005.12.084. Epub 2006 Jan 24.


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.

MeSH terms

  • Fluorescent Dyes / metabolism*
  • Ligands
  • Nanotechnology
  • Receptors, Histamine H3 / metabolism*
  • Spectrometry, Fluorescence


  • Fluorescent Dyes
  • Ligands
  • Receptors, Histamine H3