The Relationship of Anticholinesterase Activity, Penetration, and Insect and Mammalian Toxicity of Certain Organophosphorus Insecticides1

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Abstract
A study was made to correlate the in vitro inhibition of white rat (Rattus norvegicus) brain and house fly (Musca domestica L.) head cholinesterase with mammalian and insect toxicity in a series of organophosphorus compounds. The permeability of the insect integument was also studied by comparing the insecticidal activity of these compounds by injection and topical application. The results indicated the following: (1) All of the compounds tested had some ability to inhibit cholinesterase demon in vitro, but the best inhibitors were not always the most active compounds against insects or mammals. Conversely, some of the more active compounds against insects or mammals were very poor in vitro cholinesterase inhibitors. (2) The integument of the German cockroach hindered the penetration of malathion, malaoxon, and a few analogs of dimethoate. It did not hinder the penetration of isomalathion, dimethoate, and most of the analogs of dimethoate.

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