Azelastine HCl

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Chemical Structure| 79307-93-0 同义名 : 氮卓斯汀盐酸盐 ;Azelastine (hydrochloride);Azelastine hydrochloride;Azeptin;Rhinolast;Allergodil;Optivar;Astelin
CAS号 : 79307-93-0
货号 : A341055
分子式 : C22H25Cl2N3O
纯度 : 98%
分子量 : 418.359
MDL号 : MFCD00242783
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(119.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 6.5 mg/mL(15.54 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Histamine receptor
描述 Azelastine Hydrochloride is an effective, rapid-acting, and well-tolerated second-generation antihistamine that improves nasal symptoms associated with SAR (seasonal allergic rhinitis) and VMR (vasomotor rhinitis). Azelastine hydrochloride (azelastine) nasal spray is a histamine receptor-1 (H1) antagonist often used in treating allergic rhinitis to relieve its symptoms. Addition of azelastine at doses of 1μM or above elicited a significant dilation response to 1μM methoxamine-induced mucosal contraction. Azelastine could inhibit electrical field stimulation-induced spike mucosal contraction. Moreover, increase in concentration of azelastine had minimal effect on basal tension of nasal mucosa[3]. The treatment with the use of the combination of azelastine hydrochloride and mometasone furoate resulted in a more pronounced alleviation of rhinological symptoms and improvement of the quality of life at the early stages of therapy in comparison with mometasone furoate monotherapy[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.20mL

23.90mL

4.78mL

2.39mL
参考文献

[1]Hide I, Toriu N, et al. Suppression of TNF-alpha secretion by azelastine in a rat mast (RBL-2H3) cell line: evidence for differential regulation of TNF-alpha release, transcription, and degranulation. J Immunol. 1997 Sep 15;159(6):2932-40.

[2]Yoneda K, Yamamoto T, et al. Suppression by azelastine hydrochloride of NF-kappa B activation involved in generation of cytokines and nitric oxide. Jpn J Pharmacol. 1997 Feb;73(2):145-53.

[3]Cheng LH, Lee JC, Wu PC, Lin YY, Chu YH, Wang HW. Azelastine nasal spray inhibiting sympathetic function on human nasal mucosa in patients with allergy rhinitis. Rhinology. 2019 Aug 1;57(4):268-272

[4]Karpishchenko SA, Kolesnikova OM. Éffektivnost' kombinatsii azelastina gidrokhlorida i mometazona furoata dlia intranazal'nogo primeneniia u bol'nykh sezonnym allergicheskim rinitom [The effectiveness of the combination of azelastine hydrochloride and mometasone furoate for the intranasal application in the patients presenting with seasonal allergic rhinitis]. Vestn Otorinolaringol. 2017;82(5):44-47. Russian