For research use only.
CAS No. 132-17-2
Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
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|Description||Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.|
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. 
|In vivo||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. |
-  Simoni D, et al. J Med Chem, 2005, 48(9), 3337-3343.
-  Reith ME, et al. J Biol Chem, 2001, 276(31), 29012-29018.
-  Chen N, et al. J Neurochem, 2004, 89(4), 853-864.
|In vitro||Water||81 mg/mL (200.72 mM)|
|Ethanol||81 mg/mL (200.72 mM)|
|DMSO||50 mg/mL (123.9 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00715377||Terminated||Drug: Benztropine||Schizophrenia|Schizoaffective Disorder|Schizophreniform Disorder|Delusional Disorder|Psychotic Disorders||Centre for Addiction and Mental Health||June 2007||Not Applicable|
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