ChemicalBook CAS DataBase List 1056596-82-7

1056596-82-7

Name	Mizolastine (dihydrochloride)
CAS	1056596-82-7
Molecular Formula	C24H27Cl2FN6O
Molecular Weight	468.96
MOL File	1056596-82-7.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Powder

Hazard Information

Uses

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.

storage

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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