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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.
分子量 | 306.32 |
公式 | C13H16N2O.C2H2O4 |
储存 | Desiccate at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: Proxyfan oxalate, Proxyfan oxalate supplier, High, affinity, H3, ligands, Receptors, Histamine, histaminergic, 2477, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Proxyfan oxalate 的部分引用包括:
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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