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Submit ReviewThioperamide
Description: H3 antagonist; also H4 inverse agonist
Chemical Name: N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide
Purity: ≥99% (HPLC)
Biological Activity for Thioperamide
Thioperamide 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.
Technical Data for Thioperamide
| M. Wt | 292.44 |
| Formula | C15H24N4S |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 106243-16-7 |
| PubChem ID | 3035905 |
| InChI Key | QKDDJDBFONZGBW-UHFFFAOYSA-N |
| Smiles | S=C(NC3CCCCC3)N(CC2)CCC2C1=CNC=N1 |
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.
Solubility Data for Thioperamide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 29.24 | 100 | |
| ethanol | 29.24 | 100 |
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 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 |
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Product Datasheets for Thioperamide
References for Thioperamide
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
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
Do you know of a great paper that uses Thioperamide from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Histamine Receptors Scientific Review
Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.
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