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)).

In vitro inhibition of cholinesterases by carbamates--a kinetic study.

Kinetics and mechanism of in vitro hydrolyses of acetylcholine and acetylthiocholine by carbamates were studied in a batch reactor at 25 degrees C, pH 8, and ionic strength of 0.11 M. Every hydrolysis was monitored by 3-4 independent methods.