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Anatabine dicitrate

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MCE 站：Anatabine dicitrate

产品活性：Anatabine dicitrate 是一种烟草生物碱，可以穿过血脑屏障。Anatabine dicitrate 是一种有效的 α4β2 nAChR 激动剂。Anatabine dicitrate 通过阻止淀粉样蛋白前体蛋白的 β 裂解，抑制 NF-κB 激活，并降低淀粉样 β (Aβ) 的产生。Anatabine dicitrate 具有抗炎作用，可用于神经退行性疾病的研究。

研究领域：NF-κB  |  Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：NF-κB  |  Amyloid-β  |  nAChR

In Vitro: Anatabine (600 μg/mL; 24 hours; SHSY-5Y cells) treatment shows an inhibition of p65 NF-κB phosphorylation.
Anatabine (500-1000μg/mL; 30 minutes; SHSY-5Y cells) treatment fully prevents the increase in BACE-1 mRNA levels induced by TNF-α. After 24 hours, Anatabine treatment shows a dose-dependent inhibition of BACE-1 protein levels.
Anatabine dose dependently inhibits Aβ_1-40 and Aβ_1-42 with an approximate half maximal inhibitory concentration of 640 μg/mL for both Aβ_1-40 and Aβ_1-42 in 7W CHO cells. Anatabine inhibits sAPPβ secretion without impacting sAPPα suggesting that Anatabine is preventing the β-cleavage of amyloid precursor protein (APP).

In Vivo: Anatabine (0.5-2 mg/kg; intraperitoneal injection; daily; for 4 days; transgenic mouse) treatment significantly lowers brain soluble Aβ_1-40 and Aβ_1-42 levels in a transgenic mouse model of Alzheimer´s disease.

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