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125602-71-3

中文名称 贝托斯汀
英文名称 BEPOTASTINE
CAS 125602-71-3
分子式 C21H25ClN2O3
分子量 388.89
MOL 文件 125602-71-3.mol
更新日期 2024/05/22 10:40:36
125602-71-3 结构式 125602-71-3 结构式

基本信息

中文别名
贝托司汀
贝托斯汀
(+)-BEPOTASTINE
BEPOTASTINE >
90%
4-[4-[(4-氯苯基)吡啶-2-基甲氧基]哌啶-1-基]丁酸
英文别名
BEPOTASTINE
Bepotastine >
Bepotastine >90%
betotastine besilate
Bepotastine free base
-4-(4-((4-Chlorophenyl)
(190786-43-7) bepotastine
4-[(S)-(4-chlorophenyl)-2-pyridinylMethoxy]-
4-(4-[(1S)(4-CHLOROPHENYL)-2-PYRIDYLMETHOXY]PIPERIDYL)BUTANOIC ACID
4-[4-[(4-Chlorophenyl)pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
所属类别
生物化工:激动剂抑制剂

物理化学性质

熔点56 - 58°C
沸点546.8±50.0 °C(Predicted)
密度1.26
储存条件-20°C Freezer, Under inert atmosphere
溶解度可溶于DMSO(少许)、甲醇(少许)
酸度系数(pKa)4.44±0.10(Predicted)
形态固体
颜色白色至浅米色

常见问题列表

生物活性
Bepotastine是一种非镇静的、选择性histamine 1 (H1) receptor拮抗剂。
靶点

Histamine H1 receptor

体外研究

Bepotastine possesses additional anti-allergic activity including stabilization of mast cell function, inhibition of eosinophilic infiltration, inhibition of IL-5 production, and inhibition of leukotriene B4 (LTB4) and LTD4 activity.
Bepotastine significantly inhibits antigen-induced stimulation of IL-5 production in human peripheral blood mononuclear cells (PBMCs) at concentrations of 10-100 μM and the effect is enhanced when the PBMCs are pre-incubated with Bepotastine.
Leukotriene B4 increased Ca2+ concentration in cultured neutrophils, which is suppressed by Bepotastine besilate (1-100 μM). Leukotriene B4 increased Ca2+ concentration in cultured dorsal root ganglion neurons, which is also suppressed by Bepotastine besilate (100 μM).

体内研究

Bepotastine besilate (10 mg/kg) inhibits scratching induced by an intradermal injection of histamine (100 nmol/site), but not serotonin (100 nmol/site).
Bepotastine besilate (1-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B4 (0.03 nmol/site). Bepotastine in vivo dose-dependently inhibits the acceleration of histamine-induced vascular permeability and inhibits homologous passive cutaneous anaphylaxis in guinea pig studies.
In mouse models of itching, oral Bepotastine inhibits the frequency and duration of scratching behavior.

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