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Zanapezil free base

CAS No. : 142852-50-4

MCE 站：Zanapezil free base

产品活性：Zanapezil (TAK-147) free base 是一种有效、可逆和选择性的乙酰胆碱酯酶 (AChE) 抑制剂。Zanapezil free base 有效抑制大鼠大脑皮层匀浆中 AChE 活性 (IC₅₀=51.2 nM)。Zanapezil free base 适度抑制毒蕈碱 M1 和 M2 受体，K_i 值分别为 234 和 340 nM。Zanapezil free base 可用于阿尔茨海默症早期阶段的研究。

研究领域：Neuronal Signaling

作用靶点：AChE

In Vitro: Zanapezil (TAK-147) free base shows a potent ａnd reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM), ａnd is 3.0- ａnd 2.4-fold more potent than tacrine ａnd physostigmine, respectively. Zanapezil free base is the least potent inhibitor of butyrylcholinesterase activity in rat plasma (IC₅₀=23,500 nM).
Zanapezil free base moderately inhibits uptake of noradrenaline ａnd serotonin with IC₅₀ values of 4020 ａnd 1350 nM, respectively.
Zanapezil free base also inhibits ligand binding at alpha-1, alpha-2 ａnd serotonin 2 receptors with K_i values of 324, 2330 ａnd 3510 nM, respectively.

In Vivo: Oral administration of Zanapezil (TAK-147; 3 mg/kg) free base significantly accelerated the turnover rates of dopamine, noradrenaline ａnd serotonin in the rat brain. Oral administration of Zanapezil free base at doses ranging from 1 to 10 mg/kg induces a statistically significant ａnd dose-dependent decrease in AChE activity in the cerebral cortex in ex vivo experiments.
Zanapezil (TAK-147; 5 ａnd 10 mg/kg) free base significantly increases ACh level in the ventral hippocampus (VH) for 120 min.

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