263248-42-6

263248-42-6 structure

Name: Zanapezil
Chemical Name: 3-(1-Benzyl-4-piperidinyl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin- 8-yl)-1-propanone (2E)-2-butenedioate (1:1)
CAS Number: 263248-42-6
Molecular Formula: C₂₉H₃₆N₂O_5.xC₄H₄O₄
Molecular Weight: 492.60700
Catalog: Signaling Pathways Neuronal Signaling AChE
Create Date: 2016-11-24 15:42:15
Modify Date: 2024-01-10 19:25:24
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD)[1][2].

Name	3-(1-Benzyl-4-piperidinyl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin- 8-yl)-1-propanone (2E)-2-butenedioate (1:1)

Description	Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD)[1][2].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> AChE
Target	AChE
References	[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.