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) shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM), and is 3.0- and 2.4-fold more potent than tacrine and physostigmine, respectively. Zanapezil is the least potent inhibitor of butyrylcholinesterase activity in rat plasma (IC₅₀=23,500 nM)^[1].
Zanapezil moderately inhibits uptake of noradrenaline and serotonin with IC₅₀ values of 4020 and 1350 nM, respectively^[1].
Zanapezil also inhibits ligand binding at alpha-1, alpha-2 and serotonin 2 receptors with K_i values of 324, 2330 and 3510 nM, respectively^[1].

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

Oral administration of Zanapezil (TAK-147; 3 mg/kg) significantly accelerated the turnover rates of dopamine, noradrenaline and serotonin in the rat brain. Oral administration of Zanapezil at doses ranging from 1 to 10 mg/kg induces a statistically significant and dose-dependent decrease in AChE activity in the cerebral cortex in ex vivo experiments^[1].
Zanapezil (TAK-147; 5 and 10 mg/kg) significantly increases ACh level in the ventral hippocampus (VH) for 120 min^[2].

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

492.61

C₂₉H₃₆N₂O₅

142852-51-5

O=C(C1=CC=C2CCCCNC2=C1)CCC3CCN(CC4=CC=CC=C4)CC3.O=C(O)/C=C/C(O)=O

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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]