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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[1][2][3]. | [in vivo]
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[2]. | Animal Model: | Male Sprague-Dawley rats (specific-pathogen-free; 234-254 g; 7 to 8-week-old; rat paw edema model)[2]. | | 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.
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Store at -20°C | [References]
[1] Xia Q, et al. The effect of mizolastine on expression of vascular endothelial cell growth factor, tumour necrosis factor-alpha and keratinocyte-derived chemokine in murine mast cells, compared with dexamethasone and loratadine. Clin Exp Dermatol. 2005 Mar DOI:10.1111/j.1365-2230.2005.01721.x
[2] Ren X, et al. The anti-inflammatory effects of Yunnan Baiyao are involved in regulation of the phospholipase A2/arachidonic acid metabolites pathways in acute inflammation rat model. Mol Med Rep. 2017 Oct;16(4):4045-4053. DOI:10.3892/mmr.2017.7104
[3] Prakash A, et al. Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria. BioDrugs. 1998 Jul;10(1):41-63. DOI:10.2165/00063030-199810010-00004 |
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