Zanapezil  (Synonyms: TAK-147)

Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD)^[1][2].

Zanapezil (TAK-147) 对大鼠大脑皮层匀浆中的 AChE 活性具有有效且可逆的抑制作用 (IC₅₀=51.2 nM)，其效力比 Tacrine 和 Physostigmine 强 3.0 倍和 2.4 倍。Zanapezil 是大鼠血浆中丁酰胆碱酯酶活性最弱的抑制剂 (IC₅₀=23,500 nM)^[1]。
Zanapezil 中度抑制去甲肾上腺素和血清素的摄取，IC₅₀ 值分别为 4020 和 1350 nM^[1]。
Zanapezil 还抑制 α-1、α-2 和血清素 2 受体上的配体结合，K_i 值分别为 324、2330 和 3510 nM^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Zanapezil (TAK-147) (TAK-147；3 mg/kg；po) 显著加速大鼠大脑中多巴胺、去甲肾上腺素和血清素的周转率。在离体实验中，Zanapezil (TAK-147) (1-10 mg/kg; po) 会导致大脑皮层 AChE 活性出现统计学上显着的剂量依赖性下降^[1]。
Zanapezil (TAK-147) (TAK-147；5 和 10 mg/kg；po) 可显著增加腹侧海马 (VH) 的 AChE 水平，持续 120 分钟^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

492.61

C₂₉H₃₆N₂O₅

142852-51-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. K Hirai, et al. Neurochemical effects of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-b enzazepin-8-yl)-1-propanone fumarate (TAK-147), a novel acetylcholinesterase inhibitor, in rats. J Pharmacol Exp Ther. 1997 Mar;280(3):1261-9.  [Content Brief]

  [2]. Izzettin Hatip-Al-Khatib,et al. Comparison of the effect of TAK-147 (zanapezil) and E-2020 (donepezil) on extracellular acetylcholine level and blood flow in the ventral hippocampus of freely moving rats. Brain Res. 2004 Jun 25;1012(1-2):169-76.  [Content Brief]