but-2-enedioic acid
- CAS No.
- 142852-51-5
- Chemical Name:
- but-2-enedioic acid
- Synonyms
- but-2-enedioic acid;{2-[(4-chlorophenyl)(pyridin-2-yl)methoxy]ethyl}dimethylamine, 1 g;{2-[(4-chlorophenyl)(pyridin-2-yl)methoxy]ethyl}dimethylamine, 250 mg;1-Propanone, 3-(1-(phenylmethyl)-4-piperidinyl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)-,(E)-2-butenedioate (1:1)
- CBNumber:
- CB72130315
- Molecular Formula:
- C29H36N2O5
- Molecular Weight:
- 116.07
- MDL Number:
- MOL File:
- 142852-51-5.mol
| form | Solid |
|---|---|
| color | White to off-white |
| FDA UNII | 7Y1T8FKO1V |
but-2-enedioic acid Chemical Properties,Uses,Production
Uses
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].
Definition
ChEBI: Zanapezil fumarate is a polymer.
in vivo
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].
IC 50
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. PMID:9067312
[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. DOI:10.1016/j.brainres.2004.03.067