Benztropine mesylate

SKU: orb1308934

Description

Benztropine mesylate

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 132-17-2
• MW: 403.53
• Purity: 98.41%
• Formula: C₂₁H₂₅NO·CH₄SO₃
• SMILES: [C@H]12N([C@H](C[C@H](C1)OC(c1ccccc1)c1ccccc1)CC2)C.CS(=O)(=O)O
• Target: AChR,Dopamine Receptor,Histamine Receptor
• Solubility: Ethanol:75 mg/mL (185.86 mM);H2O:74 mg/mL (183.38 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.96 mM);DMSO:45 mg/mL (111.52 mM)

Bioactivity

• Target IC50:
  DAT:118 nM
• In Vivo:
  In HEK-293 cells treated with [3H]CFT and unde 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).
• In Vitro:
  At doses of 5 mg/kg and 25 mg/kg, Benztropine increase 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 o the Unified Parkinson's Disease Rating Scale without causing adverse effects such as leukopenia.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

transporter, Inhibitor, Histamine Receptor, HistamineReceptor, inhibit, Muscarinic acetylcholine receptor, mAChR, Parkinson's, anti-histamine, anticholinergic, Dopamine Receptor, Dopamine, dopamine, DopamineReceptor, disease, DAT, Benztropine, Benztropine Mesylate, Benztropine mesylate, Benztropine methanesulfonate, Benzotropine, Benzotropine mesylate, Benzotropine Mesylate, Benzatropine, Benzatropine mesylate, Benzatropine Mesylate

Compound Identifiers

PubChem CID

3246155