Affordable Access

deepdyve-link
Publisher Website

Reactivation of alkylphosphate inhibited acetylcholinesterase by bis quaternary derivatives of 2-PAM and 4-PAM

Authors
  • Wilson, Irwin B.
  • Ginsburg, Sara
Type
Published Article
Journal
Biochemical Pharmacology
Publisher
Elsevier
Publication Date
Jan 01, 1958
Volume
1
Issue
3
Pages
200–206
Identifiers
DOI: 10.1016/0006-2952(59)90099-1
Source
Elsevier
License
Unknown

Abstract

Symmetrical and unsymmetrical bis-quaternary derivatives of 2-PAM and 4-PAM were synthesized and studied as reactivators in vitro of acetylcholinesterase inhibited by TEPP and DFP. Certain of the 2-PAM-derivatives and all of the 4-PAM-derivatives were far superior to the parent compound in the sense of producing reactivations at lower concentrations. Despite the fact that 2-PAM is much more active than 4-PAM, the bis-quaternary derivatives of the latter were considerably more active in regard to DFP inhibition, but only slightly more active in regard to TEPP inhibition. The best compound with regard to DFP inhibition was the unsymmetrical bisquaternary salt of 4-PAM and pyridine with a pentamethylene linking chain. In general, the addition of extra binding features in these series produced better reactivators.

Report this publication

Statistics

Seen <100 times