Chlorpheniramine Maleate (C09-0822-609)

InformationChlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is anhistamine H1receptor antagonist withIC50of 12 nM.In vitroChlorpheniramine inhibits the [3H]mepyramine binding to the histamine H1 receptor in guinea pig cortex with IC50 of 8.8 nM. Chlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM. Chlorpheniramine displaces of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM. Chlorpheniramine treatment in human salivary gland cells more significantly inhibits the histamine-induced [Ca2+]i increase in a concentration-dependent manner with IC50 of 128 nM than that of carbachol-induced [Ca2+]i increase with an IC50 of 43.9 μM.In vivoOral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg. Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus. Administration of Chlorpheniramine (20 mg/kg) significantly abolishes the increase in REM sleep in rats induced by immobilization stress due to the blockage of the histaminergic and cholinergic mechanisms generating REM sleep.Cell Datacell lines：Hormone refractory prostate cancer cell lines (PC-3, PPC-1, DU145, TSU-Pr1 and 22Rv1) and malignant melanoma cell lines (SK-MEL-5 and A375)Concentrations：Dissolved in water, final concentrations ~500 μMIncubation Time：48 hoursPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C16H19ClN2·C4H4O4 Molecular Weight: 390.86