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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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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.
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Keywords: Thioperamide, Thioperamide supplier, H4, inverse, agonists, H3, antagonists, Receptors, Histamine, histaminergic, 0644, Tocris Bioscience
4 Citations for Thioperamide
Citations are publications that use Tocris products. Selected citations for Thioperamide include:
Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753 PMID: 21873469
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
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
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
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.