Zanapezil

Modify Date: 2024-01-10 19:25:24

Zanapezil Structure
Zanapezil structure
Common Name Zanapezil
CAS Number 263248-42-6 Molecular Weight 492.60700
Density N/A Boiling Point 547ºC at 760mmHg
Molecular Formula C29H36N2O5.xC4H4O4 Melting Point N/A
MSDS N/A Flash Point 284.6ºC

 Use of Zanapezil


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].

 Names

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

 Zanapezil Biological Activity

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
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.  

 Chemical & Physical Properties

Boiling Point 547ºC at 760mmHg
Molecular Formula C29H36N2O5.xC4H4O4
Molecular Weight 492.60700
Flash Point 284.6ºC
Exact Mass 492.26200
PSA 106.94000
LogP 5.09760
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