Proxyfan oxalate is a high affinity histamine H3 receptor ligand (pKi = 8.62) that acts as a protean (shape changing) agonist at recombinant and native receptors. This compound's functional activity ranges from full agonist to inverse agonist depending on the system used. Proxyfan oxalate 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. Baldi et al (2005) The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat. Neuropharmacology 48 246. Krueger et al (2005) G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations. J.Pharmacol.Exp.Ther 314 271.
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