[Effector modelling of the action of ligands of the GABA-receptor complex, cooperativity of the processes and the type of modification of the complex by convulsants and their reversible agonists].
The expression of cooperativity of pharmacological effects of convulsants--exogenic ligands of supramolecular GABA-receptor-channel ensemble (GABA-RC)--bicuculline, picrotoxin, pentylenetetrazole, bemegride at intravenous infusion to intact animals and against a background of administration of barbital-Na and phenazepam is determined. The supposed mechanism of bemegride effect is discussed. Analysis of principles of GABA-RC functioning in vivo on the base of pharmacological data (cooperativity coefficients and types of modulation of GABA-RC functions at the interaction of convulsants and their reverse agonists) suggests the formation of biosystem response at modification of structures adequate to one of four subunits of "quartet" (tetrameric) model of GABA-RC.
Golovenko
N Ia
NIa
Zhuk
O V
OV
Zin'kovskiĭ
V G
VG
D000818:Animals; D014151:Anti-Anxiety Agents; D000927:Anticonvulsants / Q000494:pharmacology*; D001462:Barbital / Q000494:pharmacology; D001534:Bemegride / Q000494:pharmacology; D001569:Benzodiazepines; D001570:Benzodiazepinones / Q000494:pharmacology; D001640:Bicuculline / Q000494:pharmacology; D003292:Convulsants / Q000494:pharmacology*; D004347:Drug Interactions; D005260:Female; D008024:Ligands; D008433:Mathematics; D051379:Mice; D008808:Mice, Inbred CBA; D008954:Models, Biological; D010433:Pentylenetetrazole / Q000494:pharmacology; D010852:Picrotoxin / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001462:Barbital; D001534:Bemegride; D001569:Benzodiazepines; D001570:Benzodiazepinones; D001640:Bicuculline; D003292:Convulsants; D008024:Ligands; D010433:Pentylenetetrazole; D010852:Picrotoxin; D011963:Receptors, GABA-A; C017928:phenazepam
Effektornoe modelirovanie deĭstviia ligandov GAMK-retseptornogo kompleksa, kooperativnost' protsessov i tip modifikatsii kompleksa sudorozhnymi agentami i ikh obratnymi agonistami.