Catalog Number: 0644
Chemical Name: N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide
Biological Activity
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. Also available as part of the Histamine H3 Receptor Tocriset™.
Technical Data
  • M.Wt:
    292.44
  • Formula:
    C15H24N4S
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    106243-16-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Characterization of histamine-H3 receptors in guinea pig ileum with H3-selective ligands.
    Hew et al.
    Br.J.Pharmacol., 1990;101:621
  2. Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation.
    Ling et al.
    Br.J.Pharmacol., 2004;142:161
  3. Compared pharmacology of human H3 and H4 receptors: structure-activity relationships of histamine derivatives.
    Gbahou et al.
    Br.J.Pharmacol., 2006;147:744
  4. Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow.
    Liu et al.
    Mol. Pharmacol., 2001;59:420
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Thioperamide include:

4 Citations: Showing 1 - 4
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  1. Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma.
    Authors: Francis Et al.
    Gut 2012;61:753
  2. Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells.
    Authors: Holden Et al.
    Saudi J Biol Sci 2007;152:891
  3. Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype.
    Authors: Takahashi Et al.
    J Clin Invest 2002;110:1791
  4. Activation of the p38 and p42/p44 mitogen-activated protein kinase families by the histamine H(1) receptor in DDT(1)MF-2 cells.
    Authors: Robinson and Dickenson
    Br J Pharmacol 2001;133:1378

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