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Benztropine mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Benztropine mesylate图片
CAS NO:132-17-2
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)403.53
FormulaC21H25NO.CH4SO3
CAS No.132-17-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 50 mg/mL (123.9 mM)
Water: 81 mg/mL (200.7 mM)
Ethanol: 81 mg/mL (200.7 mM)
Other info

Chemical Name: (1R,3r,5S)-3-(benzhydryloxy)-8-methyl-8-azabicyclo[3.2.1]octane methanesulfonate

InChi Key: CPFJLLXFNPCTDW-BWSPSPBFSA-N

InChi Code: InChI=1S/C21H25NO.CH4O3S/c1-22-18-12-13-19(22)15-20(14-18)23-21(16-8-4-2-5-9-16)17-10-6-3-7-11-17;1-5(2,3)4/h2-11,18-21H,12-15H2,1H3;1H3,(H,2,3,4)/t18-,19+,20+;

SMILES Code: CN1[C@@H]2C[C@@H](OC(C3=CC=CC=C3)C4=CC=CC=C4)C[C@H]1CC2.OS(C)(=O)=O

Synonyms

NSC42199; ST50997629; NSC-42199; ST-50997629; NSC 42199; ST 50997629; Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate; Benztropine Mesylate; Cogentin; Cogentin mesylate; MLS000737056

实验参考方法
In Vitro

In vitro activity: Benztropine inhibits MTSET-induced inhibition of [3H]WIN binding to Wild-type dopamine transporter with EC50 of 28 μM in concentration-dependent manner. Benztropine has a protective ratio (EC50/inhibiting [3H]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 [3H]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 [3H]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.


Kinase Assay:


Cell Assay:

In VivoBenztropine (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.
Animal model
Formulation & Dosage
References

J Med Chem. 2005 May 5;48(9):3337-43; Neurology. 1997 Apr;48(4):1077-81.