Cat. No. 2477
Chemical Name: 4-[3-(Phenylmethoxy)propyl]-1H-imid
Biological ActivityHigh 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Baldi et al (2005) The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat. Neuropharmacology 48 246. PMID: 15695163.
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. PMID: 15821027.
Gbahou et al (2003) Protean agonism at histamine H3 receptors in vitro and in vivo. Proc.Natl.Acad.Sci.USA 100 11086.
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Citations are publications that use Tocris products. Selected citations for Proxyfan oxalate include:
Singh et al (2012) Development of time-resolved fluorescent based [EU]-GTP binding assay for selection of human Histamine 3 receptor antagonists/inverse agonist: a potential target for Alzheimer's treatment. Ann Neurosci 19 71. PMID: 25205969.
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Keywords: Proxyfan oxalate, supplier, High, affinity, H3, ligands, Receptors, Histamine, histaminergic, Tocris Bioscience, Histamine H3 Receptor Agonist products