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Literature summary for 3.1.1.7 extracted from

  • Zhang, J.; Zhu, D.; Sheng, R.; Wu, H.; Hu, Y.; Wang, F.; Cai, T.; Yang, B.; He, Q.
    BZYX, a novel acetylcholinesterase inhibitor, significantly improved chemicals-induced learning and memory impairments on rodents and protected PC12 cells from apoptosis induced by hydrogen peroxide (2009), Eur. J. Pharmacol., 613, 1-9.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(E)-2-(4-[(diethylamino)methyl]benzylidene)-5,6-dimethoxy-2,3-dihydroinden-1-one i.e. BZYX, an indanone derivative, and a dual-binding-site AChE inhibitor. BZYX also shows high neuroprotection from H2O2-induced apoptosis in PC12 cells and prevents loss of membrane potential, determination with fluorescent 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazol-carbocyanine iodide, i.e. JC-1, overview Rattus norvegicus
donepezil
-
Rattus norvegicus
galanthamine
-
Rattus norvegicus
huperzine A
-
Rattus norvegicus
rivastigmine
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain cortex
-
Rattus norvegicus
-
PC-12 cell
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Rattus norvegicus acetate + thiocholine
-
?

Synonyms

Synonyms Comment Organism
AChE
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000019
-
pH 7.4, 37°C Rattus norvegicus donepezil
0.000053
-
pH 7.4, 37°C Rattus norvegicus huperzine A
0.000058
-
pH 7.4, 37°C Rattus norvegicus (E)-2-(4-[(diethylamino)methyl]benzylidene)-5,6-dimethoxy-2,3-dihydroinden-1-one
0.00301
-
pH 7.4, 37°C Rattus norvegicus galanthamine
0.00381
-
pH 7.4, 37°C Rattus norvegicus rivastigmine