Mizolastine - CAS 108612-45-9
Catalog number: 108612-45-9
Category: Inhibitor
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Molecular Formula:
C24H25FN6O
Molecular Weight:
432.49
COA:
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Targets:
Histamine Receptor
Description:
Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
Purity:
>98%
Synonyms:
Mizollen; SL 850324; SL850324; SL-850324; Mistalin; Mistamine; Mizolastina; Mizolastine
MSDS:
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InChIKey:
PVLJETXTTWAYEW-UHFFFAOYSA-N
InChI:
InChI=1S/C24H25FN6O/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32)
Canonical SMILES:
CN(C1CCN(CC1)C2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)F)C5=NC=CC(=O)N5
1.Influence of component 5a receptor 1 (C5AR1) -1330T/G polymorphism on nonsedating H1-antihistamines therapy in Chinese patients with chronic spontaneous urticaria.
Yan S1, Chen W1, Wen S2, Zhu W1, Guo A1, Chen X3, Zhang C1, Chen M1, Zhang J1, Su J1, Zhao Y1, He Y1, Liu Z3, Zhou H3, Zeng W1, Li J4, Chen X5. J Dermatol Sci. 2014 Dec;76(3):240-5. doi: 10.1016/j.jdermsci.2014.09.012. Epub 2014 Oct 8.
BACKGROUND: The nonsedating H1-antihistamines are the first-line medicines for chronic spontaneous urticaria (CSU) patients. However, not all these patients respond well to the antihistamines, and the mechanisms underlying the interindividual differences are still unclear. C5AR1 gene encodes the component 5a receptor (C5aR) protein, which has been reported to play an important role in chronic spontaneous urticaria.
2.Cetirizine and loratadine: minimal risk of QT prolongation.
Prescrire Int. 2010 Feb;19(105):26-8.
Some antihistamines, such as mizolastine and ebastine, can prolong the QT interval and provoke severe cardiac arrhythmias. This review examines the effects of two widely used antihistamines, cetirizine and loratadine, on the QT interval. As of mid 2009 very few clinical data had been published on the risk of QT prolongation with cetirizine or loratadine. The very rare reported cases of torsades de pointes linked to loratadine mainly appear to involve drug interactions, especially with amiodarone and enzyme inhibitors. We found no reports of QT prolongation attributed to desloratadine, the main metabolite of loratadine. Two cases of QT prolongation with cetirizine have been published, one of which involved overdose and renal failure. The reports are too vague to conclude that cetirizine was implicated. We found no reports of QT prolongation attributed to levocetirizine. Cetirizine is a metabolite of hydroxyzine, another antihistamine. In the 1960s, a study of patients with psychosis showed a risk of QT prolongation.
3.Efficacy of second-generation antihistamines in patients with allergic rhinitis and comorbid asthma.
Bachert C1, Maspero J. J Asthma. 2011 Nov;48(9):965-73. doi: 10.3109/02770903.2011.616616. Epub 2011 Oct 4.
BACKGROUND AND AIMS: Allergic rhinitis (AR) and asthma share common mediators, cytokines, and chemokines from mast cells and basophils that are central to the complex cascade of events involved in the inflammatory response. Histamine is the salient mediator released after immunologic challenge, initiating multiple pathologic processes of the allergic reaction that result in bronchial smooth muscle contraction, vasodilation, mucus hypersecretion, and edema. The recent identification of a fourth histamine receptor has reinforced clinical interest in the pleiotropic effects of histamine and the relative roles of histamine receptors in mediating immune and inflammatory responses.
4.Trace analysis of three antihistamines in human urine by on-line single drop liquid-liquid-liquid microextraction coupled to sweeping micellar electrokinetic chromatography and its application to pharmacokinetic study.
Gao W1, Chen Y, Chen G, Xi J, Chen Y, Yang J, Xu N. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Sep 1;904:121-7. doi: 10.1016/j.jchromb.2012.07.032. Epub 2012 Aug 3.
A rapid and efficient dual preconcentration method of on-line single drop liquid-liquid-liquid microextraction (SD-LLLME) coupled to sweeping micellar electrokinetic chromatography (MEKC) was developed for trace analysis of three antihistamines (mizolastine, chlorpheniramine and pheniramine) in human urine. Three analytes were firstly extracted from donor phase (4 mL urine sample) adjusted to alkaline condition (0.5 M NaOH). The unionized analytes were subsequently extracted into a drop of n-octanol layered over the urine sample, and then into a microdrop of acceptor phase (100 mM H(3)PO(4)) suspended from a capillary inlet. The enriched acceptor phase was on-line injected into capillary with a height difference and then analyzed directly by sweeping MEKC. Good linear relationships were obtained for all analytes in a range of 6.25 × 10(-6) to 2.5 × 10(-4)g/L with correlation coefficients (r) higher than 0.987. The proposed method achieved limits of detections (LOD) varied from 1.
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CAS 108612-45-9 Mizolastine

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