| Name | Benztropine mesylate |
| 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. |
| 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). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 74 mg/mL (183.38 mM), Sonication is recommended.
DMSO : 45 mg/mL (111.52 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.96 mM), Sonication is recommended.
Ethanol : 75 mg/mL (185.86 mM), Sonication is recommended.
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| Keywords | transporter | Parkinson's | Muscarinic acetylcholine receptor | mAChR | Inhibitor | inhibit | HistamineReceptor | Histamine Receptor | DopamineReceptor | Dopamine Receptor | dopamine | Dopamine | disease | DAT | Benztropine Mesylate | Benztropine mesylate | Benztropine | Benzotropine Mesylate | Benzotropine | Benzatropine Mesylate | Benzatropine | anti-histamine | anticholinergic |
| Inhibitors Related | Undecane | Adiphenine hydrochloride | Meclizine dihydrochloride | Urethane | Famotidine | Adenine | Sodium butanoate | Mitotane | Creatine | N,N-Dicyclohexylcarbodiimide | Arecoline | Alginic acid |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
