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The toxic action of some phosphorus anticholinesterases with cationic groups

Authors
  • Heath, D.F.
Type
Published Article
Journal
Biochemical Pharmacology
Publisher
Elsevier
Publication Date
Jan 01, 1961
Volume
6
Issue
4
Pages
244–251
Identifiers
DOI: 10.1016/0006-2952(61)90137-X
Source
Elsevier
License
Unknown

Abstract

The intravenous LD 50 in rats and I 50 to sheep AChE of several compounds of the type (RO) 2PO·S·CH 2·CH 2·Z have been determined. Z represents SR, RR' or, in one case, R 3, where the R's are alkyl groups. Special precautions had to be taken to get reliable values. The LD 50 and I 50 of the cationic compounds are very much lower than those of their uncharged analogues. Two of the sulphonium compounds are the most toxic phosphorus anti-AChE's reported. The results are discussed in terms of the mechanism of inhibition at the enzyme surface.

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