甲磺酸苯扎托品，Benztropine mesylate；≥99.0%(HPLC)

A brain penetrating azabicyclo[3.2.1]octane derivative with anti-cholinergic and anti-histaminergic properties. Acts as an antagonist of muscarinic M1 and M3 receptors induces robust differentiation of oligodendrocytes precursor cell differentiation (OPC; EC₅₀ = 500 nM) and promotes myelination. Reduces the expression of Notch 1 in immature OPC and reduces the levels of cyclin D1 and D2 and c-Fos and c-Jun indicating its inhibitory effect on cell cycle progression. Shown to reduce the severity of the acute phase of multiple sclerosis and virtually eliminates the relapse phase in animal models. Significantly reduces the severity in the experimental autoimmune encephalomyelitis (EAE) model of relapsing-remitting multiple sclerosis when administered alone or co-administered with FTY720 (Cat. No. 344597).

 

一种具有抗胆碱能和抗组胺能特性的脑穿透性氮杂双环 [3.2.1] 辛烷衍生物。 作为毒蕈碱 M1 和 M3 受体的拮抗剂，可诱导少突胶质细胞前体细胞分化 (OPC；EC50 = 500 nM) 的强烈分化并促进髓鞘形成。 降低未成熟 OPC 中 Notch 1 的表达并降低细胞周期蛋白 D1 和 D2 以及 c-Fos 和 c-Jun 的水平，表明其对细胞周期进程的抑制作用。 在动物模型中显示可降低多发性硬化症急性期的严重程度并几乎消除复发期。 当单独给药或与 FTY720（货号 344597）共同给药时，显着降低复发缓解型多发性硬化症实验性自身免疫性脑脊髓炎 (EAE) 模型的严重程度。

 

Cell permeable: yes

Reversible: yes

Primary Target
Muscarinic M1/M3

 

Packaged under inert gas

 

Toxicity: Toxic (F)

 

Deshmukh, V.A, et al. 2013. Nature 502,327.
Doshay, L.J., et al. 1956. J Am Med Assoc.162, 1031.

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