Bilastine selectively antagonizes histamine H1 receptor and it is used to treat allergic rhinoconjunctivitis and urticaria.
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产品名称 | H1 receptor ↓ ↑ | H2 receptor ↓ ↑ | H3 receptor ↓ ↑ | H4 receptor ↓ ↑ | Histamine receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Hydroxyzine 2HCl | 99+% | ||||||||||||||||||
Cyclizine | ✔ | 97% | |||||||||||||||||
Loratadine |
+
B(0)AT2, IC50: 4 μM |
98% | |||||||||||||||||
Desloratadine |
++
Histamine H1 receptor, IC50: 51 nM |
98% | |||||||||||||||||
Doxylamine succinate | ✔ | 99% | |||||||||||||||||
Ebastine | ✔ | 98% | |||||||||||||||||
Tripelennamine HCl |
+
H1 receptor, IC50: 30 μM |
98% | |||||||||||||||||
Meclizine dihydrochloride | ✔ | 98% | |||||||||||||||||
Chlorpheniramine maleate |
+++
Histamine H1 receptor, IC50: 12 nM |
99% | |||||||||||||||||
Diphenhydramine HCl | ✔ | 99% | |||||||||||||||||
Alcaftadine |
++++
H1 receptor, pKi: 8.5 |
++
H2 receptor, pKi: 7.2 |
99%+ | ||||||||||||||||
Fexofenadine HCl |
++
Histamine H1 receptor, IC50: 246 nM |
99%+ | |||||||||||||||||
Bilastine |
+++
H1 receptor, Ki: 44.15 nM |
98% | |||||||||||||||||
Pemirolast potassium | ✔ | 98% | |||||||||||||||||
Bepotastine besilate |
+
Histamine H1 receptor, pIC50: 5.7 |
98% | |||||||||||||||||
Mizolastine |
+++
Histamine H1 receptor, IC50: 47 nM |
98% | |||||||||||||||||
Brompheniramine maleate | ✔ | 98% | |||||||||||||||||
Carbinoxamine maleate salt | ✔ | 99+% | |||||||||||||||||
Clemastine fumarate |
++++
Histamine H1 receptor, IC50: 3 nM |
98% | |||||||||||||||||
Ketotifen fumarate salt | ✔ | 95% | |||||||||||||||||
Rupatadine Fumarate |
++
Histamine H1 receptor, Ki: 102 nM |
PAFR | 98% | ||||||||||||||||
Famotidine | ✔ | 97% | |||||||||||||||||
Roxatidine Acetate HCl |
+
Histamine H2 receptor, IC50: 3.2 μM |
98% | |||||||||||||||||
Lafutidine | ✔ | 99% | |||||||||||||||||
Cimetidine | ✔ | 98% | |||||||||||||||||
Nizatidine |
++++
Histamine H2 receptor, IC50: 0.9 nM |
AChE | 98% | ||||||||||||||||
Ranitidine | ✔ | 98% | |||||||||||||||||
Betahistine |
+
Histamine H3 receptor, IC50: 1.9 μM |
98% | |||||||||||||||||
Ciproxifan maleate |
+++
Histamine H3 receptor, IC50: 9.2 nM |
99%+ | |||||||||||||||||
S 38093 |
++
human H3 receptor, Ki: 1.2 μM rat H3 receptor, Ki: 1.44 μM |
98% | |||||||||||||||||
JNJ-7777120 |
++++
Histamine H4 receptor, Ki: 4.5 nM |
98% | |||||||||||||||||
Azelastine HCl | ✔ | 98% | |||||||||||||||||
Epinastine HCl | ✔ | 98% | |||||||||||||||||
Levodropropizine | ✔ | 97% | |||||||||||||||||
Cyproheptadine hydrochloride | ✔ | 98% | |||||||||||||||||
Hesperetin | ✔ | 97% | |||||||||||||||||
Olopatadine HCl | ✔ | 98% | |||||||||||||||||
Mianserin hydrochloride | ✔ | 99+% | |||||||||||||||||
Buclizine 2HCl | ✔ | 97% | |||||||||||||||||
Latrepirdine 2HCl | ✔ | GluR | 98% | ||||||||||||||||
Cetirizine 2HCl | ✔ | 98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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]. |
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 | - | - |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 202189-78-4 |
分子式 | C28H37N3O3 |
分子量 | 463.612 |
别名 | F-96221-BM1 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
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 |