ワモンゴキブリにおけるNS 2662 (<i>O</i>, <i>O</i>-dimethyl 2, 2-dichloro 1-hydroxyethyl phosphonate)の代謝ならびにコリンエステラーゼ阻害

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  • Metabolism and Cholinesterase Inhibition of NS 2662, <i>O</i>, <i>O</i>-dimethyl 2, 2-dichloro 1-hydroxyethyl phosphonate, in the American cockroach
  • ワモンゴキブリ ニ オケル NS2662 O , O-dimethyl 2 , 2-dichloro 1-hydroxyethyl phosphonate ノ タイシャ ナラビニ コリンエステラーゼ ソガイ

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The mammalian toxicity of NS 2662, O, O-dimethyl 2, 2-dichloro 1-hydroxyethyl phosphonate, is very low. Toxic symptoms on the mouse caused by this new insecticide are quite different from those caused by other organophosphorus compounds. During the present studies, the mode of action of the new compound in the American cockroach was investigated. The distribution 32P-NS 2662 and 32P-trichlorfon in the American cockroach was investigated. High concentrations of radioactive materials have been found in the nerve cord, guts and muscles of paralyzed insects, compared with normal tissues. Very small amounts of radioactive materials were found in the nerve tissues. The concentrations of NS 2662 and trichlorfon in the abdominal nerve cord of paralyzed insect were suggested to be less than 10-5 and 10-6 M respectively. Both insecticides were degraded rapidly to water soluble metabolites by the cockroach. About 30 and 50% of doses were recovered as chloroform soluble radioactive materials one and 24 hours after the topical application of 32P-NS 2662, respectively. In case of 32P-trichlorfon application, these figures were about 60 and 15%. The main water soluble degradation products were O, O-dimethyl phosphoric acid, desmethyl-DMVP, monomethyl phosphoric acid and phosphoric acid in the former case, and phosphoric acid, desmethyl-dichlorvos, monomethyl phosphoric acid and O, O-dimethyl phosphoric acid in the latter one. An active metabolite, DMVP (O, O-dimethyl 2-monochlorovinyl phosphate) or dichlorvos, was found less than three percent of the doses. IN 50 values of the insecticides for abdominal nerve cord ChE in the cockroach were as follows: NS 2662, 7.8×10-6M, DMVP, 7.1×10-7M, trichlorfon, 9.3×10-6M and dichlorvos, 2.1×10-7M. The in vivo inhibition of ChE activity in the cockroach was measured. No symptoms were observed until about 50% of ChE activity was inhibited. At the convulsive and paralyzed stages, the inhibition of ChE activity was about 80 and 90% respectively. The above results suggest that ChE is the target of NS 2662 in the cockroach. NS 2662 and DMVP, the vinyl derivative of NS 2662, may play a role in ChE inhibition.

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