Thioperamide

Key Product Details

Product Description

Thioperamide is a potent histamine H₃ and H₄ antagonist/inverse agonist. K_i 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.

Product Specifications for Thioperamide

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Thioperamide

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.42 mL	17.10 mL	34.20 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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 48 publications citing the usage of this product.

• Liu Cloning and pharmacological characterization of a fourth histamine receptor (H₄) expressed in bone marrow. Mol. Pharmacol. 2001 PMID: 11179434
• Hew Characterisation of histamine H₃ receptors in guinea pig ileum with H₃ selective ligands. Br.J.Pharmacol. 1990 PMID: 1963802
• Ling Histamine H₄ receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br.J.Pharmacol. 2004 PMID: 15131002
• Gbahou Compared pharmacology of human H₃ and H₄ receptors: structure-activity relationships of histamine derivatives. Br.J.Pharmacol. 2006 PMID: 16432504

Product Documents for Thioperamide