Thioperamide dot maleate CAS: 148440-81-7
MF: C15H24N4S•C4H4O4
MW: 408.5
A potent and selective histamine H3 receptor antagonist shown to cross the blood-brain barrier.

Thioperamide·maleate (CAS 148440-81-7)

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Synonym: N-cyclohexyl-4-(1H-imidazol-5-yl)-1-piperidinecarbothioamide, 2Z-butenedioate
Application: A potent and selective histamine H3 receptor antagonist shown to cross the blood-brain barrier
CAS Number: 148440-81-7
Purity: ≥98%
Molecular Weight: 408.5
Molecular Formula: C15H24N4S•C4H4O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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Thioperamide·maleate is a selective histamine H3 receptor antagonist and H4 receptor inverse agonist that has been shown to cross the blood-brain barrier. This compound binds to rat cerebral cortical cells in vitro, has a pKi value of 8.4. Additionally, thioperamide maleate blocks eosinophil shape change (IC50 = 1.4 μM) and chemotaxis (IC50) = 519 nM) induced by histamine.


References

1. Arrang, J.M., et al. 1987. Nature. 327: 117-123. PMID: 3033516
2. LaBella, F.S., et al. 1992. Br. J. Pharmacol. 107: 161-164. PMID: 1330158
3. Meier, G., et al. 2001. Eur J Pharm Sci. 13: 249-259. PMID: 11384847
4. Harada, C., et al. 2004. Brain Res. Bull. 63: 143-146. PMID: 15130703
5. Fogel, W.A., et al. 2007. Inflamm. Res. 56: S21-S22. PMID: 17806163
6. Welty, N., et al. 2009. Psychopharmacology. 207: 433-438. PMID: 19795107
7. Jośko, J., et al. 2010. Neurotox Res. [Epub ahead of print]. PMID: 20838953

Physical State :
Solid
Solubility :
Soluble in water (50 mM), DMSO (100 mM), and ethanol (100 mM).
Storage :
Desiccate at 4° C
IC50 :
eosinophil shape change: IC50 = 1.4 µM; chemotaxis: IC50 = 519 nM
Ki Data :
recombinant H 3: Ki= 25 nM (human); recombinant H 4: Ki= 27 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
53393972
SMILES :
C1CCC(CC1)NC(=S)N2CCC(CC2)C3=CN=CN3.C(=CC(=O)O)C(=O)O

Download SDS (MSDS)

Certificate of Analysis

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