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Submit ReviewThioperamide is a potent histamine H3 and H4 antagonist/inverse agonist. Ki values are 25 and 27 nM for human recombinant H3 and H4 receptors respectively. Blocks eosinophil shape change (IC50 = 1.4 μM) and chemotaxis (IC50 = 519 nM) induced by histamine. Freely crosses the blood-brain barrier.
分子量 | 292.44 |
公式 | C15H24N4S |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 106243-16-7 |
PubChem ID | 3035905 |
InChI Key | QKDDJDBFONZGBW-UHFFFAOYSA-N |
Smiles | S=C(NC3CCCCC3)N(CC2)CCC2C1=CNC=N1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 29.24 | 100 | |
ethanol | 29.24 | 100 |
以下数据基于产品分子量 292.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.42 mL | 17.1 mL | 34.2 mL |
5 mM | 0.68 mL | 3.42 mL | 6.84 mL |
10 mM | 0.34 mL | 1.71 mL | 3.42 mL |
50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
参考文献是支持产品生物活性的出版物。
Gbahou et al (2006) Compared pharmacology of human H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br.J.Pharmacol. 147 744 PMID: 16432504
Hew et al (1990) Characterisation of histamine H3 receptors in guinea pig ileum with H3 selective ligands. Br.J.Pharmacol. 101 621 PMID: 1963802
Ling et al (2004) Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br.J.Pharmacol. 142 161 PMID: 15131002
Liu et al (2001) Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59 420 PMID: 11179434
If you know of a relevant reference for Thioperamide, please let us know.
关键词: Thioperamide, Thioperamide supplier, H4, inverse, agonists, H3, antagonists, Receptors, Histamine, histaminergic, 0644, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Thioperamide 的部分引用包括:
Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753 PMID: 21873469
Robinson and Dickenson (2001) Activation of the p38 and p42/p44 mitogen-activated protein kinase families by the histamine H(1) receptor in DDT(1)MF-2 cells. Br J Pharmacol 133 1378 PMID: 11498525
Takahashi et al (2002) Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest 110 1791 PMID: 12488429
Holden et al (2007) Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells. Saudi J Biol Sci 152 891 PMID: 17891168
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