[Interaction with esterases and mechanism of synergistic action of thio- and dithiophosphates containing the fragments of N-acylated glycine and beta-alanine].
We studied the interaction between O,O-diethyl-S-[(N-acyl-N-alkoxycarbonylalkyl)aminomethyl]thiophosphates and mammalian cholinesterases as well as esterases from insect tissue extracts by kinetic methods and disc electrophoresis. The coefficients of combined effect of these compounds or their dithioanalogs with permethrin were determined. The obtained data suggest that the synergistic effect on the common cockroaches and houseflies is chiefly due to carboxylesterase inhibition by monothioderivatives and monooxygenase suppression by dithioderivatives, respectively.
Khrunin
A V
AV
Moscow State Pedagogical University, Malaya Pirogovskaya ul. 1, Moscow, 119882 Russia.
Eremina
O Iu
OIu
Bakanova
E I
EI
Roslavtseva
S A
SA
Shipov
A E
AE
Genkina
G K
GK
Mastriukova
T A
TA
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D003058:Cockroaches / Q000201:enzymology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004357:Drug Synergism; D004950:Esterases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D005998:Glycine / Q000737:chemistry*; D006793:Houseflies / Q000201:enzymology; D006801:Humans; D007306:Insecticides / Q000737:chemistry* / Q000494:pharmacology*; D007928:Lethal Dose 50; D008297:Male; D008322:Mammals; D009946:Organothiophosphorus Compounds; D013329:Structure-Activity Relationship; D015091:beta-Alanine / Q000737:chemistry*
D002800:Cholinesterase Inhibitors; D007306:Insecticides; D009946:Organothiophosphorus Compounds; D015091:beta-Alanine; D004950:Esterases; D005998:Glycine