Chemical Name:4-[3-(Phenylmethoxy)propyl]-1H-imidazole maleate
Biological Activity:
High affinity histamine H3 receptor
ligand (pKi = 8.62) that acts as a protean agonist at recombinant
and native receptors. In functional studies, activity ranges from full agonist
to inverse agonist depending on system used. Displays partial agonist effects
on cAMP inhibition and MAPK activity, neutral antagonist activity on histamine
release and partial inverse agonism of [3H]-arachidonic acid
release.
Gbahou et al
(2003) Protean agonism at histamine H3 receptors in vitro and
in vivo. Proc.Natl.Acad.Sci.USA 100 11086. Baldiet
al (2005) The H3 receptor protean agonist proxyfan enhances the
expression of fear memory in the rat. Neuropharmacology 48 246. Kruegeret al (2005) G protein-dependent pharmacology of histamine H3
receptor ligands: evidence for heterogeneous active state receptor
conformations. J.Pharmacol.Exp.Ther 314 271.