Benztropine mesylate

SKU: orb1308934

Description

Benztropine mesylate is a centrally acting muscarinic antagonist and dopamine reuptake inhibitor. It is used in research models of Parkinson's disease, primarily to study cholinergic-dopaminergic interactions in both in vitro binding assays and in vivo behavioral experiments.

Research Area

Immunology & Inflammation, Neuroscience

Key Properties

• CAS Number: 132-17-2
• MW: 403.53
• Purity: >98%
• Formula: C₂₁H₂₅NO CH₄SO₃
• SMILES: [C@H]12N([C@H](C[C@H](C1)OC(c1ccccc1)c1ccccc1)CC2)C.CS(=O)(=O)O
• Target: Monoamine transporter
• Solubility: Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 5 mg/ml with warming)

Bioactivity

• Target IC50:
  DAT:118 nM
• 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).
• 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.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• 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