"目錄號: HY-14602

Neuronal Signaling-

Tramiprosate是一個(gè)小的，能夠口服的化合物，可以結(jié)合可溶性Aβ，減少淀粉樣蛋白聚合和隨后的沉積。

Amyloid-β

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生物活性

Description

Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent depositiontarget: AβIn vitro: Tramiprosate provides neuroprotection against? Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors. Tramiprosate dose-dependently provides neuroprotection against ischemic stroke.In vivo: Tramiprosate produced dose-dependent reductions of Aβ in the brain of transgenic mice (hAPP-TgCRND8). Clinical studies show that tramiprosate was safe and tolerable. In mild-to-moderate AD patients tramiprosate also reduced Aβ42 levels in CSF.The reference for animal administration is 50 mg/kg.

Clinical Trial

NCT00314912

Bellus Health Inc

Alzheimer's Disease

May 2006

Phase 3

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References

[1].Wu S et al. Tramiprosate protects neurons against ischemic stroke by disrupting the interaction between PSD95 and nNOS. Neuropharmacology. 2014 Aug;83:107-17.

[2].Aisen PS et al. Tramiprosate in mild-to-moderate Alzheimer's disease - a randomized, double-blind, placebo-controlled, multi-centre study (the Alphase Study). Arch Med Sci. 2011 Feb;7(1):102-11.