Proxyfan oxalate

Biological Activity

Proxyfan oxalate is a high affinity histamine H₃ receptor ligand (pK_i = 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. The H₃ receptor protean agonist proxyfan enhances the expression of fear memory in the rat.
   Baldi et al.
   Neuropharmacology, 2005;48:246
2. G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations.
   Krueger et al.
   J.Pharmacol.Exp.Ther, 2005;314:271
3. Protean agonism at histamine H₃ receptors in vitro and in vivo.
   Gbahou et al.
   Proc.Natl.Acad.Sci.USA, 2003;100:11086

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