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抑制劑描述：

產(chǎn)品名稱：Benztropine mesylate

產(chǎn)品別名：甲磺酸苯扎托品

英文別名：Benzatropine mesylate;Benzotropine mesylate;Benztropine methanesulfonate

靶點：DAT

CAS：132-17-2

純度：>98%

外觀：見愛必信官網(wǎng)

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Benztropine抑制MTSET誘導的[³H]WIN與野生型多巴胺轉運蛋白結合的抑制，EC50為28 μM且具有濃度依賴特性。Benztropine對X-A342C DAT的保護率(EC50/抑制[³H]WIN (4nM)結合的IC50)為32，這是通過保護DAT342號半胱氨酸實現(xiàn)的。 在沒有鈉鹽時W84L DAT對Benztropine的表觀平衡解離常數(shù)明顯高于野生型DAT，這種差異在[³H]CFT處理的HEK-293細胞并含有130 mM鈉鹽條件下變小了。

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

體外研究：

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.

體內(nèi)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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