Benztropine mesylate

For research use only.

Catalog No.S3163

Benztropine mesylate Chemical Structure

Molecular Weight(MW): 403.53

Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.

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10mM (1mL in DMSO) USD 200 In stock
USD 97 In stock
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Biological Activity

Description Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
Targets
DAT [1]
118 nM
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 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]

Protocol

Solubility (25°C)

In vitro Water 81 mg/mL (200.72 mM)
Ethanol 81 mg/mL (200.72 mM)
DMSO 50 mg/mL (123.9 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 403.53
Formula

C21H25NO.CH4SO3

CAS No. 132-17-2
Storage powder
in solvent
Synonyms N/A
Smiles CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4.C[S](O)(=O)=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID