产品说明书

Bilastine

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Chemical Structure| 202189-78-4 同义名 : F-96221-BM1
CAS号 : 202189-78-4
货号 : A325945
分子式 : C28H37N3O3
纯度 : 98%
分子量 : 463.612
MDL号 : MFCD09837814
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(19.41 mM)，配合低频超声，并水浴加热至45℃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
动物实验配方：
生物活性
靶点

  • H1 receptor

    H1 receptor, Ki:44.15 nM
描述 Bilastine is a potent and highly selective H1-antihistamine approved for the treatment of allergic rhinoconjunctivitis and urticaria. Bilastine is a suitable option for the treatment of patients with allergic rhinoconjunctivitis or urticaria across age groups from school-age children to elderly patients[3]. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity[4]. Bilastine 20 mg once daily (therapeutic dose) is non-sedating, does not enhance the effects of alcohol or CNS sedatives, does not impair driving performance and has at least similar efficacy as other second-generation H1-antihistamines in the treatment of allergic rhinoconjunctivitis and urticaria[5]. With respect to somnolence, bilastine is a substrate for P-glycoprotein, a membrane pump which prevents it crossing the blood-brain barrier[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02557269 Seasonal Allergic Rhinitis Phase 4 Unknown December 2015 Bulgaria ... 展开 >> Medical University Sofia, University Hospital "Alexandrovska", Clinic of Allergy and Asthma Sofia, Bulgaria, 1431 收起 <<
NCT01940393 Urticaria Phase 4 Completed - Colombia ... 展开 >> Medellin Medellin, Antioquia, Colombia 收起 <<
NCT00421109 Urticaria Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.78mL

2.16mL

1.08mL

21.57mL

4.31mL

2.16mL
参考文献

[1]Jauregizar N, de la Fuente L, et al. Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet. 2009;48(8):543-54.

[2]Corcostegui R, Labeaga L, et al. Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D. 2005;6(6):371-84.

[3]Church MK, Tiongco-Recto M, Ridolo E, Novák Z. Bilastine: a lifetime companion for the treatment of allergies. Curr Med Res Opin. 2020 Mar;36(3):445-454

[4]Wang XY, Lim-Jurado M, Prepageran N, Tantilipikorn P, Wang de Y. Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine. Ther Clin Risk Manag. 2016 Apr 13;12:585-97

[5]Jáuregui I, Ramaekers JG, Yanai K, Farré M, Redondo E, Valiente R, Labeaga L. Bilastine: a new antihistamine with an optimal benefit-to-risk ratio for safety during driving. Expert Opin Drug Saf. 2016 Jan;15(1):89-98

[6]Church MK, Labeaga L. Bilastine: a new H1 -antihistamine with an optimal profile for updosing in urticaria. J Eur Acad Dermatol Venereol. 2017 Sep;31(9):1447-1452