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编 号：F023609
分子式：C24H27Cl2FN6O
分子量：505.42
分子式：C24H27Cl2FN6O
分子量：505.42
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CAS No: 1056596-82-7
产品详情
生物活性：
Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial.
体内研究：
Mizolastine dihydrochloride (0.3 mg/kg; p.o.; single daily for 7 days) inhibits production of 5-LOX AA (arachidonic acid) metabolite leukotriene B4 (LTB4), and suppresses expression of 5-LOX, cytosolic PLA2 (cPLA2), 5-LOX-activating protein, and LTB4 receptor mRNA in the AA-induced inflammation model.Animal Model:Male Sprague-Dawley rats (specific-pathogen-free; 234-254 g; 7 to 8-week-old; rat paw edema model).
Dosage:0.3 mg/kg
Administration:Oral gavage; single daily for 7 days.
Result:Significantly reduced paw edema by 21% at 1 h, and by 14?18% between 2 and 4 h.Inhibited inflammatory cell infiltration and significantly reduced levels of LTB4.Suppressed expression of 5?LOX, cPLA2, FLAP and LTB4r mRNA.
体外研究：
Mizolastine dihydrochloride (1-10000 nM; 0.5-6 h) shows inhibitory effects on VEGF, KC and TNF-α release in mast cells.Mizolastine dihydrochloride (0.1 μM; 4 h) significantly reduces VEGF165, VEGF120, TNF-α and KC mRNA expression in mast cells.
Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial.
体内研究：
Mizolastine dihydrochloride (0.3 mg/kg; p.o.; single daily for 7 days) inhibits production of 5-LOX AA (arachidonic acid) metabolite leukotriene B4 (LTB4), and suppresses expression of 5-LOX, cytosolic PLA2 (cPLA2), 5-LOX-activating protein, and LTB4 receptor mRNA in the AA-induced inflammation model.Animal Model:Male Sprague-Dawley rats (specific-pathogen-free; 234-254 g; 7 to 8-week-old; rat paw edema model).
Dosage:0.3 mg/kg
Administration:Oral gavage; single daily for 7 days.
Result:Significantly reduced paw edema by 21% at 1 h, and by 14?18% between 2 and 4 h.Inhibited inflammatory cell infiltration and significantly reduced levels of LTB4.Suppressed expression of 5?LOX, cPLA2, FLAP and LTB4r mRNA.
体外研究：
Mizolastine dihydrochloride (1-10000 nM; 0.5-6 h) shows inhibitory effects on VEGF, KC and TNF-α release in mast cells.Mizolastine dihydrochloride (0.1 μM; 4 h) significantly reduces VEGF165, VEGF120, TNF-α and KC mRNA expression in mast cells.
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