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Inhibition of Cholinesterase by Dialkylcarbamates

Author:
Šárka Štĕpánková, Karel Komers, Alena Komersová, Markéta Masopustová, Alexander Čegan
Source:
Zeitschrift für Naturforschung 2014 v.62 no.3-4 pp. 308-310
ISSN:
0939-5075
Subject:
Alzheimer disease, blood-brain barrier, cholinesterase, drugs, enzyme activity
Abstract:
The pI₅₀ index and separation coefficients of chosen 3-N,N-diethylaminophenyl-N′,N′-dialkylcarbamates were determined. Index pI₅₀ (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 (Kₒw). Obtained results were compared with pI₅₀ and Kₒw of Exelon®, the commercially used drug against the Alzheimer’s disease.
Agid:
5230926