Molecular structure of Thioperamide·maleate, CAS Number: 148440-81-7
Thioperamide·maleate (CAS 148440-81-7)
Alternate Names:
N-cyclohexyl-4-(1H-imidazol-5-yl)-1-piperidinecarbothioamide, 2Z-butenedioate
Application:
Thioperamide⋅maleate is 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
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
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.
Thioperamide·maleate (CAS 148440-81-7) References
- Betahistine increases vestibular blood flow. | Dziadziola, JK., et al. 1999. Otolaryngol Head Neck Surg. 120: 400-5. PMID: 10064646
- Influence of imidazole replacement in different structural classes of histamine H(3)-receptor antagonists. | Meier, G., et al. 2001. Eur J Pharm Sci. 13: 249-59. PMID: 11384847
- H3 receptor antagonist, thioperamide, inhibits adrenal steroidogenesis and histamine binding to adrenocortical microsomes and binds to cytochrome P450. | LaBella, FS., et al. 1992. Br J Pharmacol. 107: 161-4. PMID: 1330158
- Inhibitory effect of iodophenpropit, a selective histamine H3 antagonist, on amygdaloid kindled seizures. | Harada, C., et al. 2004. Brain Res Bull. 63: 143-6. PMID: 15130703
- H3 histamine receptor agonist inhibits biliary growth of BDL rats by downregulation of the cAMP-dependent PKA/ERK1/2/ELK-1 pathway. | Francis, H., et al. 2007. Lab Invest. 87: 473-87. PMID: 17334413
- Influence of the H3/H4 receptor antagonist, thioperamide on regional haemodynamics in rats with trinitrobenzene sulfonic acid-induced colitis. | Fogel, WA., et al. 2007. Inflamm Res. 56 Suppl 1: S21-2. PMID: 17806163
- The effects of thioperamide on extracellular levels of glutamate and GABA in the rat prefrontal cortex. | Welty, N. and Shoblock, JR. 2009. Psychopharmacology (Berl). 207: 433-8. PMID: 19795107
- Antihistaminic drugs modify casein-induced inflammation in the rat. | Rzodkiewicz, P., et al. 2010. Inflamm Res. 59 Suppl 2: S187-8. PMID: 20012883
- Thioperamide, an H₃ receptor antagonist prevents [³H]glucose uptake in brain of adult rats lesioned as neonates with 5,7-dihydroxytryptamine. | Jośko, J., et al. 2011. Neurotox Res. 20: 93-6. PMID: 20838953
- Lymphatic diamine oxidase secretion stimulated by fat absorption is linked with histamine release. | Ji, Y., et al. 2013. Am J Physiol Gastrointest Liver Physiol. 304: G732-40. PMID: 23413254
- Highly potent and selective ligands for histamine H3-receptors. | Arrang, JM., et al. Nature. 327: 117-23. PMID: 3033516
- Role of histamine in rodent antinociception. | Malmberg-Aiello, P., et al. 1994. Br J Pharmacol. 111: 1269-79. PMID: 8032614
- H1-receptor-mediated excitation and facilitation of the heat response by histamine in canine visceral polymodal receptors studied in vitro. | Koda, H., et al. 1996. J Neurophysiol. 76: 1396-404. PMID: 8890260
Inhibitor of:
Histamine H3 Receptor, and Histamine H4 Receptor.Activator of:
Histamine H4 Receptor.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Thioperamide·maleate, 10 mg | sc-201092 | 10 mg | $102.00 | |||
Thioperamide·maleate, 50 mg | sc-201092A | 50 mg | $449.00 |