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Benztropine mesylate

Catalog No. T1336   CAS 132-17-2
Synonyms: Benzotropine mesylate, Benzatropine mesylate, Benztropine methanesulfonate

Benztropine mesylate (Benztropine methanesulfonate) is a centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.

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Benztropine mesylate Chemical Structure
Benztropine mesylate, CAS 132-17-2
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500 mg In stock $ 29.00
1 mL * 10 mM (in DMSO) In stock $ 30.00
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Purity: 100%
Purity: 99.52%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Benztropine mesylate (Benztropine methanesulfonate) is a centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.
Targets&IC50 DAT:118 nM
In vitro At doses of 5 mg/kg and 25 mg/kg, Benztropine increases the levels of extracellular dopamine in the striatum of rats in a dose-dependent manner. A daily dose of 3 mg of Benztropine effectively improves tremor and motor scores in patients with Parkinson's disease on the Unified Parkinson's Disease Rating Scale without causing adverse effects such as leukopenia.
In vivo In HEK-293 cells treated with [3H]CFT and under the condition of 130 mM sodium ions, the D313N DAT exhibited a slight increase in the apparent equilibrium dissociation constant for Benztropine. The double mutant W84L D313N DAT showed a similar apparent equilibrium dissociation constant for Benztropine when compared to the single mutation. Benztropine inhibited MTSET-induced binding of [3H]WIN to the wild-type dopamine transporter with an EC50 of 28 μM in a concentration-dependent manner. Furthermore, Benztropine demonstrated a protection rate of 32 in the X-A342C DAT construct by shielding Cys-342 from reactivity (EC50 for inhibition of [3H]WIN (4 nM) to IC50 binding).
Synonyms Benzotropine mesylate, Benzatropine mesylate, Benztropine methanesulfonate
Molecular Weight 403.53
Formula C21H25NO·CH4SO3
CAS No. 132-17-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 74 mg/mL (183.4 mM)

DMSO: 47 mg/mL (116.5 mM)

Ethanol: 75 mg/mL (185.9 mM)

TargetMolReferences and Literature

1. Simoni D, et al. J Med Chem, 2005, 48(9), 3337-3343. 2. Reith ME, et al. J Biol Chem, 2001, 276(31), 292012-292018. 3. Chen N, et al. J Neurochem, 2004, 89(4), 853-864. 4. Friedman JH, et al. Neurology, 1997, 48(4), 1077-10781. 5. Church WH, et al. Eur J Pharmacol, 1987, 139(3), 345-348.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Obesity Compound Library Bioactive Compounds Library Max Endocrinology-Hormone Compound Library

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Keywords

Benztropine mesylate 132-17-2 GPCR/G Protein Immunology/Inflammation Neuroscience Dopamine Receptor AChR Histamine Receptor Benzotropine mesylate Benzatropine mesylate Benzotropine Benzotropine Mesylate disease Benzatropine anti-histamine Inhibitor inhibit Benztropine methanesulfonate Benztropine Muscarinic acetylcholine receptor Parkinson's anticholinergic mAChR Benzatropine Mesylate Benztropine Mesylate dopamine transporter inhibitor

 

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