title: [The role of the blockade of separate subtypes of muscarinic receptors in realizing the antidotal effect of m-cholinolytics in dimethyl dichlorovinyl phosphate poisoning].
abstract: On comparison of the values of receptor selectivity of a series of m-cholinoblockers in vitro with those of the selectivity of their effect in in vivo experiments, pharmacological tests characterizing the interaction of ligands with m1, m2, and m3-subtypes of muscarine receptors were determined. Analysis of the protective effect of m-cholinoblockers in poisoning with organophosphorus compounds (OPC) depending on their activity in the determined tests showed that blocking of the m1-cholinoceptors is responsible for the antidotal effect of the antagonists, whereas block ing of m2-cholinoceptors prevents it. It is suggested that the negative effect of m2-cholinoceptor blocking on the protective effect of the drugs in OPC poisoning is mediate d by increased excretion of the mediator into the synaptic cleft as a result of interaction of the ligands with the presynaptic autochol inoceptors.
authors.affiliation: Institute of Toxicology, Ministry of Public Health, St. Petersburg, Russia.
authors.forename: A B
authors.initials: AB
authors.lastname: Kosmachev
authors.forename: V A
authors.initials: VA
authors.lastname: Beliaev
authors.forename: O A
authors.initials: OA
authors.lastname: Fil'ko
authors.forename: N P
authors.initials: NP
authors.lastname: Podosinovikova
authors.forename: N E
authors.initials: NE
authors.lastname: Solov'eva
authors.forename: T A
authors.initials: TA
authors.lastname: Titkova
mesh_terms: D000818:Animals; D000931:Antidotes / Q000627:therapeutic use*; D001921:Brain / Q000187:drug effects; D004006:Dichlorvos / Q000506:poisoning*; D004353:Drug Evaluation, Preclinical; D005260:Female; D006321:Heart / Q000187:drug effects; D007306:Insecticides / Q000506:poisoning*; D008024:Ligands; D008297:Male; D018727:Muscarinic Antagonists / Q000627:therapeutic use*; D011041:Poisoning / Q000188:drug therapy; D051381:Rats; D011976:Receptors, Muscarinic / Q000187:drug effects*; D012469:Salivary Glands / Q000187:drug effects
chemical_list: D000931:Antidotes; D007306:Insecticides; D008024:Ligands; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic; D004006:Dichlorvos