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
      Biochemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE