| Bioactivity | Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial[1][2][3]. | ||||||||||||
| Invitro | Mizolastine (1-10000 nM; 0.5-6 h) shows inhibitory effects on VEGF, KC and TNF-α release in mast cells[1].Mizolastine (0.1 µM; 4 h) significantly reduces VEGF165, VEGF120, TNF-α and KC mRNA expression in mast cells[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | Mizolastine (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: | ||||||||||||
| Name | Mizolastine | ||||||||||||
| CAS | 108612-45-9 | ||||||||||||
| Formula | C24H25FN6O | ||||||||||||
| Molar Mass | 432.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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 [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. [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. |
Mizolastine
CAS: 108612-45-9 F: C24H25FN6O W: 432.49
Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generati
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