Zanapezil

CAS: 142852-51-5 F: C29H36N2O5 W: 492.61

Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a pot

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Bioactivity	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 Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD)[1][2].
Invitro	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，Ki 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. 0 --> Zanapezil 相关抗体:
In Vivo	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.
CAS	142852-51-5
Formula	C29H36N2O5
Molar Mass	492.61
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.

Citraconic anhydride