Thioperamide (maleate) |
| Katalog-Nr.GC45045 |
Thioperamid (Maleat) (MR-12842 Maleat) ist ein potenter, oral verfügbarer, in das Gehirn eindringender und selektiver H3-Rezeptorantagonist mit einem Ki von 4,3 nM zur Hemmung der [3H]-Histaminfreisetzung.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 148440-81-7
Sample solution is provided at 25 µL, 10mM.
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Thioperamide (maleate) is a selective histamine H3 receptor antagonist that crosses the blood-brain barrier. This compound binds to rat cerebral cortical cells in vitro with a pKi value of 8.4 and inhibits histamine binding in vivo with an ED50 value of 1 mg/kg.[1] At a dose of 5 mg/kg thioperamide (maleate) inhibits kindled seizures in rats by decreasing histamine and gamma-aminobutyric acid.[2]
Reference:
[1]. Meir, G., Apelt, J., Reichert, U., et al. Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists. European Journal of Pharmaceutical Sciences 13, 249-259 (2001).
[2]. Harada, C., Fujii, Y., Hirai, T., et al. Inhibitory effect of iodophenprofit, a selective histamine H3 antagonist, on amygdaloid kindled seizures. Brain Research Bulletin 63, 143-146 (2004).
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