H3R antagonist 1 hydrochloride |
Catalog No.GC64661 |
Le chlorhydrate de l'antagoniste H3R 1 est un agoniste inverse du récepteur de l'histamine 3 (H3R) extrait du brevet WO2013107336A1, exemple composé 2.
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Cas No.: 2319790-07-1
Sample solution is provided at 25 µL, 10mM.
H3R antagonist 1 hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.
Treatment with H3R antagonist 1 hydrochloride, which is a H3R inverse agonist, promotes oligodendrocyte precursor cell (OPC) differentiation in a dose-dependent manner, at EC50=25 nM. Western blot reveals a significant increase in expression levels of two markers of mature oligodendrocytes, myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes after treatment with H3R antagonist 1 hydrochloride, which suggests that treatment with H3R antagonist 1 hydrochloride drives more OPCs to differentiate. H3R antagonist 1 hydrochloride increases the Forskolin-stimulated cAMP level in the primary oligodendrocyte precursor cells in a dose-dependent manner[1].
The ability of H3R antagonist 1 hydrochloride-1 to enhance in vivo remyelination is determined with the Cuprizone/Rapamycin-induced demyelination model. Mice are treated with Cuprizone diet combined with intraperitoneal injections of Rapamycin for 5 weeks followed by 9 days of compound administration. Cuprizone diet plus intraperitoneal injections of Rapamycin induced severe demyelination in both corpus callosum and cortex and treatment with H3R antagonist 1 hydrochloride (30 mg/kg, 9 days) significantly increases density of myelin specific Black-gold II staining in the lesion of corpus callosum and cortex in forebrain, compared to vehicle control group[1].
[1]. WANG, Rong, et al. THERAPEUTIC USES. WO2013107336A1.
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