1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Mizolastine dihydrochloride

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

Mizolastine dihydrochloride Chemical Structure

CAS No. : 1056596-82-7

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Description

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 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.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Mizolastine dihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mizolastine dihydrochloride
Cat. No.:
HY-B0164A
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