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View all Histamine H<sub>3</sub> Receptors products.Proxyfan oxalate is a 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.
M. Wt | 306.32 |
Formula | C13H16N2O.C2H2O4 |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 1620017-81-3 |
PubChem ID | 76900838 |
InChI Key | QVMZCQMJBQSPSW-UHFFFAOYSA-N |
Smiles | OC(=O)C(O)=O.C(COCC1=CC=CC=C1)CC1=CN=CN1 |
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.
References are publications that support the biological activity of the product.
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
Keywords: Proxyfan oxalate, Proxyfan oxalate supplier, High, affinity, H3, ligands, Receptors, Histamine, histaminergic, 2477, Tocris Bioscience
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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