142852-51-5
Chemical Structure
Zanapezil
Synonym(s): TAK-147
- CAS No.: 142852-51-5
- Formula:C29H36N2O5
- Molecular Weight:492.61
IUPAC Name: 3-(1-benzylpiperidin-4-yl)-1-(2,3,4,5-tetrahydro-1H-benzo[b]azepin-8-yl)propan-1-one fumarate
InChIKey: CWEHWZPCDBRUNO-WLHGVMLRSA-N
SMILES: O=C(C1=CC=C2CCCCNC2=C1)CCC3CCN(CC4=CC=CC=C4)CC3.O=C(O)/C=C/C(O)=O
Biological Activity: 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].
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Zanapezil | 99.63% | 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). | ||||||||||||||||||||
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- [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]
Keywords
