Mizolastine dihydrochloride

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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.

For research use only. We do not sell to patients.

Mizolastine dihydrochloride Chemical Structure

CAS No. : 1056596-82-7

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Other In-stock Forms of Mizolastine dihydrochloride:

Mizolastine

Other Forms of Mizolastine dihydrochloride:

Mizolastine In-stock

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

Mizolastine dihydrochloride (1-10000 nM; 0.5-6 h) shows inhibitory effects on VEGF, KC and TNF-α release in mast cells^[1].
Mizolastine dihydrochloride (0.1 µM; 4 h) significantly reduces VEGF165, VEGF120, TNF-α and KC mRNA expression in mast cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	Mast cells (from Kunming mice)
Concentration:	1-10000 nM
Incubation Time:	0.5-6 h
Result:	Markedly inhibited release of KC, VEGF and TNF-α in a time- and dose- dependent manner.

RT-PCR^[1]

Cell Line:	Mast cells (from Kunming mice)
Concentration:	0.1 µM
Incubation Time:	4 h
Result:	Led to a significant reduction of induced VEGF165, VEGF120, TNF-α and KC mRNA synthesis.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

Molecular Weight

505.42

Formula

C₂₄H₂₇Cl₂FN₆O

CAS No.

1056596-82-7

SMILES

O=C1NC(N(C2CCN(C3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C)=NC=C1.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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 [Content Brief]

[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. [Content Brief]

[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. [Content Brief]