产品说明书

Bepotastine besilate

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Chemical Structure| 190786-44-8 同义名 : Bepotastine (besylate);TAU 284
CAS号 : 190786-44-8
货号 : A307253
分子式 : C27H31ClN2O6S
纯度 : 98%
分子量 : 547.063
MDL号 : MFCD01938491
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(191.93 mM)，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

    Histamine H1 receptor, pIC50:5.7
描述 Bepotastine besilate (BB) is a second-generation H1-antihistamine that, as an ophthalmic solution, is approved in the United States by the Food and Drug Administration (FDA) for the treatment of allergic conjunctivitis. BB is effective and well-tolerated in the treatment of allergic rhinitis. Side effects are infrequent in patients with AR who do not have kidney or liver disease[3]. Bepotastine may also have other immunoactive properties, such as inhibition of eosinophil migration, interleukin-5 (IL-5), leukotrienes (e.g., LTB4) and platelet-activating factor (PAF)[4]. Bepotastine in vivo dose-dependently inhibited the acceleration of histamine-induced vascular permeability and inhibited homologous passive cutaneous anaphylaxis in guinea pig studies. In mouse models of itching, oral bepotastine inhibited the frequency and duration of scratching behavior. Multiple in vivo animal toxicology studies have demonstrated bepotastine to be safe with no significant effects on respiratory, circulatory, central nervous, digestive, or urinary systems[5].
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
NCT02686294 Rhinitis, Allergic, Perennial Phase 1 Completed - Korea, Republic of ... 展开 >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 收起 <<
NCT02682745 Rhinitis, Allergic, Perennial Phase 1 Completed - Korea, Republic of ... 展开 >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 收起 <<
NCT03200496 Healthy Phase 1 Completed - Korea, Republic of ... 展开 >> Korea University Anam Hospital Seoul, Korea, Republic of 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.14mL

1.83mL

0.91mL

18.28mL

3.66mL

1.83mL
参考文献

[1]Ohashi R, Kamikozawa Y, et al. Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate. Drug Metab Dispos. 2006 May;34(5):793-9.

[2]Da Prada M, Kettler R, et al. Neurochemical profile of moclobemide, a short-acting and reversible inhibitor of monoamine oxidase type A. J Pharmacol Exp Ther. 1989 Jan;248(1):400-14.

[3]Carrillo-Martin I, Gonzalez-Estrada A, Dimov V. Bepotastine besilate for the treatment of perennial allergic rhinitis. Expert Opin Pharmacother. 2018 Oct;19(15):1727-1730

[4]Bielory L, Duttachoudhury S, McMunn A. Bepotastine besilate for the treatment of pruritus. Expert Opin Pharmacother. 2013 Dec;14(18):2553-69

[5]Williams JI, Gow JA, Klier SM, McCue SL, Salapatek AM, McNamara TR. Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate. Curr Med Res Opin. 2010 Oct;26(10):2329-38