Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase ( AChE ) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex ( IC 50 =51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K i values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD).

Zanapezil (TAK-147) free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC 50 =51.2 nM), and is 3.0- and 2.4-fold more potent than tacrine and physostigmine, respectively. Zanapezil free base is the least potent inhibitor of butyrylcholinesterase activity in rat plasma (IC 50 =23,500 nM)[1]. Zanapezil free base moderately inhibits uptake of noradrenaline and serotonin with IC 50 values of 4020 and 1350 nM, respectively[1]. Zanapezil free base 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].

Oral administration of Zanapezil (TAK-147; 3 mg/kg) free base significantly accelerated the turnover rates of dopamine, noradrenaline and serotonin in the rat brain. Oral administration of Zanapezil free base 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) free base significantly increases ACh level in the ventral hippocampus (VH) for 120 min[2]. Animal Model: Male Wistar rats 7 weeks in age (230-240 g)[2]Dosage: 5 and 10 mg/kg Administration: Oral administration Result: Increased acetylcholine (ACh) level in the VH for 120 min.

142852-50-4

C25H32N2O

376.544

Zanapezil free base;TAK-147 free base;Zanapezil free base

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years