title: [The antagonism of phosphorus-containing heterocyclics with the anticholinesterase agent Phosphacol (paraoxon)].
abstract: Effects of 15 derivatives of 2-R-oxo-(tioxo-3,5,5-trimethyl-1,2-oxaphospholan-3-ol (OPh) on lethality and protective action on cholinesterase (ChE) of mice brain and blood serum as a result of phosphacolum (paraoxonum) poisoning were investigated. Oxo and tioxo derivatives of OPh with O-methyl and O-ethyl, but not O-propyl and O-butyl radicals at phosphoric atom prevented the lethality of mice poisoned with phosphacolum and preserved brain and blood ChE of inhibition. Ethylic and phenylic OPh derivatives also prevented the lethality of poisoned animals, although without the protection of brain and blood plasma ChE. Combined application of OPh O-ethylic derivative with atropinum and dipiroxinum significantly potentiated antidotal effect m mice poisoned by phosphacolum.
authors.forename: R S
authors.initials: RS
authors.lastname: Garaev
mesh_terms: D000818:Animals; D000931:Antidotes / Q000494:pharmacology* / Q000627:therapeutic use; D002800:Cholinesterase Inhibitors / Q000506:poisoning* / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D005260:Female; D006571:Heterocyclic Compounds / Q000494:pharmacology* / Q000627:therapeutic use; D007306:Insecticides / Q000037:antagonists & inhibitors* / Q000506:poisoning / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009943:Organophosphorus Compounds / Q000494:pharmacology* / Q000627:therapeutic use; D010261:Paraoxon / Q000037:antagonists & inhibitors* / Q000506:poisoning / Q000633:toxicity; D011041:Poisoning / Q000188:drug therapy / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D000931:Antidotes; D002800:Cholinesterase Inhibitors; D006571:Heterocyclic Compounds; D007306:Insecticides; D009943:Organophosphorus Compounds; D010261:Paraoxon
vernacular_title: Antagonizm fosforsoderzhashchikh geterotsiklov s antikholinésteraznym sredstvom fosfakolom (paraoksonom).