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抑制剂描述:

产品名称:Benztropine mesylate

产品别名:见爱必信官网

英文别名:Benztropine mesylate

靶点:AChR

CAS:132-17-2

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Benztropine抑制MTSET诱导的[³H]WIN与野生型多巴胺转运蛋白结合的抑制,EC50为28 μM且具有浓度依赖特性。Benztropine对X-A342C DAT的保护率(EC50/抑制[³H]WIN (4nM)结合的IC50)为32,这是通过保护DAT342号半胱氨酸实现的。 在没有钠盐时W84L DAT对Benztropine的表观平衡解离常数明显高于野生型DAT,这种差异在[³H]CFT处理的HEK-293细胞并含有130 mM钠盐条件下变小了。

溶解性:Ethanol :75 mg/mL (185.9 mM)
DMSO :47 mg/mL (116.5 mM)
Water :74 mg/mL (183.4 mM)

体外研究:

Benztropine inhibits MTSET-induced inhibition of WIN binding to Wild-type dopamine transporter with EC50 of 28 μM in concentration-dependent manner. Benztropine has a protective ratio (EC50/inhibiting WIN (4 nm) binding with IC50) of 32 in X-A342C DAT construct by protecting Cys-342 from reaction. The apparent equilibrium dissociation constant of W84L DAT for benztropine is significantly higher than that of WT in the absence of sodium but this difference becomes smaller in the presence of 130 mM sodium in HEK-293 cells incubated with CFT. The apparent equilibrium dissociation constant of D313N DAT for benztropine displays a modest increase in the presence of 130 mM sodium in HEK-293 cells incubated with CFT. The apparent equilibrium dissociation constant value for benztropine at the double mutant (W84L D313N DAT) is in general close to that at one of the single mutants.

体内研究:Benztropine (3.0 mg/day) is effective in improving tremor and the motor score of the United Parkinson's Disease Rating Scale without adverse events like leukopenia. Benztropine (5 mg/kg and 25 mg/kg) shows dose-dependent elevations in extracellular dopamine in the striatum of the rat.

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