product name Benztropine mesylate
Description: Benztropine is a highly potent dopamine transporter (DAT) inhibitor with IC50 of 118 nM. Benztropine is a synthetic compound derived from the combination of atropine and diphenhydramine that acts centrally to antagonize M1 muscarinic acetylcholine receptors. Benztropine has been used in the treatment of Parkinson’s disease symptoms to address involuntary tremor and dystonia. It can also increase the availability of dopamine by inhibiting uptake through the dopamine transporter.
References: J Med Chem. 2005 May 5;48(9):3337-43; Neurology. 1997 Apr;48(4):1077-81.
403.53
Formula
C21H25NO.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)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19413905
| 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 Vivo | Benztropine (3.0 mg/day) is effective in improving tremor and the motor score of the United Parkinsons 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. |
