Accession Number : ADP008853
Title : Slow, Tight-Binding Inhibition of Acetylcholinessterase (AChe) By Aryl trifluoromethyl Ketones.
Corporate Author : IOWA UNIV IOWA CITY DEPT OF CHEMISTRY
Personal Author(s) : Quinn, D. M. ; Nair, H. ; Servalli, J. ; Lee, K. ; Doctor, B. P.
Report Date : 13 MAY 1993
Pagination or Media Count : 7
Abstract : Acetylcholinesterases from Torpedo californica (TC-AChE) and Electrophorus electricus (EE-AChE) are inhibited by aryl trifluoroketones, m-XPhCOCF3. Trifluoroacetophenone (TFA; X = H) is a rapid competitive inhibitor; K(i) values are 210 nM and 520 nm for respective inhibitions of EE-AChE and TC-AChE. m-Dimethylamino trifluoroacetophenone (DMTFA, X = Me2N) and m-trimethylamino trifluoroacetophenone (TMTFA, X = Me3N+) are slow, tight binding inhibitors. The kinetics of inhibition by DMTFA are described.
Descriptors : *CHOLINESTERASE INHIBITORS, *ACETYLCHOLINESTERASE, *KETONES, INHIBITION, KINETICS, VALUE, ARYL RADICALS, FLUORINATED HYDROCARBONS, METHYL RADICALS, SHARKS, EELS.
Subject Categories : Pharmacology
Distribution Statement : APPROVED FOR PUBLIC RELEASE