Slow, Tight-Binding Inhibition of Acetylcholinessterase (AChe) By Aryl trifluoromethyl Ketones.

Quinn, D. M.; Nair, H.; Servalli, J.; Lee, K.; Doctor, B. P.

Slow, Tight-Binding Inhibition of Acetylcholinessterase (AChe) By Aryl trifluoromethyl Ketones.

Active / Technical Report | Accession Number: ADP008853 |

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 Ki 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.

Author(s):

Quinn, D. M. ; Nair, H. ; Servalli, J. ; Lee, K. ; Doctor, B. P.

Author Organization(s):

IOWA UNIV IOWA CITY DEPT OF CHEMISTRY

Supplementary Note:

This article is from 'Proceedings of the Medical Defense Bioscience Review (1993) Held in Baltimore, Maryland on 10-13 May 1993. Volume 3', AD-A275 669, p991-997.

Pagination:

0007

Security Markings

DOCUMENT & CONTEXTUAL SUMMARY

Distribution:

Approved For Public Release

RECORD

Collection: TR

Identifying Numbers

Monitor Series:

USAMRDC

Subject Terms

Joint Capability Areas:

JCA_3.2_Engagement; JCA_3_Force Application

Communities of Interest:

Weapons Technologies

Descriptor(s):

*CHOLINESTERASE INHIBITORS, *ACETYLCHOLINESTERASE, *KETONES, INHIBITION, KINETICS, VALUE, ARYL RADICALS, FLUORINATED HYDROCARBONS, METHYL RADICALS, SHARKS, EELS

Field(s)/Group(s):

Pharmacology, Biochemistry

Keyword(s):

Trifluoroacetophenone, *Aryl trifluoromethyl ketones, Acetophenone, M Dimethylamino trifluoro, Acetophenone, M Trimethylamino, Trifluoromethyl ketones, Component reports

Report Date:

1993 May 13