Inhibition of cholinesterase by dialkylcarbamates.
The pI50 index and separation coefficients of chosen 3-N,N-diethylaminophenyl-N',N'-dialkylcarbamates were determined. Index pL50 (pI50 = negative logarithm of molar concentration of inhibitor inhibiting the enzyme activity by 50%) describes the effectiveness of the inhibitor. The rate of ability of the inhibitor to pass the blood-brain barrier is usually described by the separation coefficient in a system n-octanol/water (K(ow)). Obtained results were compared with pL50 and K(ow) of Exelon, the commercially used drug against the Alzheimer's disease.
Stĕpánková
Sárka
S
Faculty of Chemical Technology, University of Pardubice, Department of Biological and Biochemical Sciences, Strossova 239, 530 03 Pardubice, Czech Republic. sarka.stepankova@upce.cz
Komers
Karel
K
Komersová
Alena
A
Masopustová
Markéta
M
Cegan
Alexander
A
D000110:Acetylcholinesterase / Q000378:metabolism*; D000122:Acetylthiocholine / Q000378:metabolism; D000478:Alkylation; D000818:Animals; D002219:Carbamates / Q000737:chemistry / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004146:Dioxanes / Q000494:pharmacology; D004593:Electrophorus; D007700:Kinetics; D008958:Models, Molecular
D002219:Carbamates; D002800:Cholinesterase Inhibitors; D004146:Dioxanes; D000122:Acetylthiocholine; D000110:Acetylcholinesterase; C025223:1,4-dioxane