Benztropine mesylate

製品コードS3163 バッチS316302

化学情報

	Synonyms	Cogentin mesylate, Benztropine methanesulfonate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₂₅NO.CH₄SO₃
	分子量	403.53	CAS No.	132-17-2
Solubility (25°C)*	体外	Water	81 mg/mL (200.72 mM)
		Ethanol	81 mg/mL (200.72 mM)
		DMSO	50 mg/mL (123.9 mM)
* <1 mg/ml means slightly soluble or insoluble. * 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.

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生物活性

製品説明	Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 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]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	Rats are decapitated and their brains are quickly removed and placed in ice-cold 0.32 M sucrose. The striatal tissue is removed and homogenized in 20 volumes of 0.32 M sucrose using a Polytron homogenizer. The supernatant obtained after centrifugation for 10 min at 0°C (S1 fraction) is removed and centrifuged for 20 min at 2×10⁴ g and 0℃ to obtain the P2 fraction, which is then resuspended in 50 volumes (original wet weight) of ice-cold 25 mM sodium phosphate buffer (pH 7.7). Samples containing phosphate buffer, P2 suspension, Benztropine, water or cocaine 50 μM (to define non-specific binding) and [³H]WIN 2 nM are incubated for 2h at 0°C.

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Food and Drug Administration-approved antipsychotic drug trifluoperazine, a calmodulin antagonist, inhibits viral replication through PERK-eIF2α axis [ Front Microbiol, 2022, 13:979904]	PubMed: 36386620

The Food and Drug Administration-approved antipsychotic drug trifluoperazine, a calmodulin antagonist, inhibits viral replication through PERK-eIF2α axis [ Front Microbiol, 2022, 13:979904]

PubMed: 36386620

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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