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Category: 7TM ReceptorsarrowHistamine ReceptorsarrowH3 and H4 ReceptorsarrowAgonists
Cat.No. Product Name
2477 Proxyfan maleate
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Proxyfan
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.

Technical Data:

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M.Wt: 332.35
Formula: C13H16N2O.C4H4O4
Storage: Desiccate at RT
Solubility: Soluble to 100 mM in DMSO
CAS No: [177708-09-7]

Resources:

  • Certificate of Analysis / MSDS:

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    Product/Material Safety Data Sheet: View current batch

    References:

    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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    Keywords: Proxyfan, Histamine Receptors, High Affinity H3 Ligand, Tocris Bioscience

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