Benztropine mesylate

Synonyms: Cogentin mesylate, Benztropine methanesulfonate

Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.

Benztropine mesylate Chemical Structure

Benztropine mesylate Chemical Structure

CAS: 132-17-2

Selleck's Benztropine mesylate has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.94%
99.94

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Biological Activity

Description Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
Targets
DAT [1]
118 nM
In vitro
In vitro

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. [2] 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. [3]

In Vivo
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. [4] Benztropine (5 mg/kg and 25 mg/kg) shows dose-dependent elevations in extracellular dopamine in the striatum of the rat. [5]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00715377 Terminated
Schizophrenia|Schizoaffective Disorder|Schizophreniform Disorder|Delusional Disorder|Psychotic Disorders
Centre for Addiction and Mental Health
June 2007 Not Applicable

Chemical Information & Solubility

Molecular Weight 403.53 Formula

C21H25NO.CH4SO3

CAS No. 132-17-2 SDF Download Benztropine mesylate SDF
Smiles CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4.CS(=O)(=O)O
Storage (From the date of receipt)

In vitro
Batch:

Water : 81 mg/mL

Ethanol : 81 mg/mL

DMSO : 50 mg/mL ( (123.9 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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