[The pharmacological selectivity of cholinesterase inhibitors is due to their antagonism with calcium ions].
The inhibitory activity of O-carbamoyl acylhydroxymoylchlorides was studied on the purified specimens of acetylcholinesterase from human erythrocytes and butirylcholinesterase from the horse blood serum. The pharmacological activity of these compounds was studied on isolated organs of rats. It was shown that introduction of N-aryl substituent in carbamate molecule increases the anticholinesterase activity and efficacy of blocking the neuromuscular conductivity. However it significantly diminishes the spasmogenic effect of N-arylcarbamates on the ileum. An increase in N-arylcarbamate concentration to 0.02-0.04 mM and higher results in a spasmolytic effect on the ileum which can be attributed to their "side" calcium blocking action.
Ivanov
Iu Ia
IuIa
D000818:Animals; D002091:Butyrylcholinesterase; D002118:Calcium / Q000037:antagonists & inhibitors*; D002219:Carbamates / Q000494:pharmacology* / Q000633:toxicity; D002800:Cholinesterase Inhibitors / Q000494:pharmacology* / Q000633:toxicity; D004305:Dose-Response Relationship, Drug; D004912:Erythrocytes / Q000187:drug effects / Q000201:enzymology; D006736:Horses; D006801:Humans; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009469:Neuromuscular Junction / Q000187:drug effects; D051381:Rats; D013329:Structure-Activity Relationship
D002219:Carbamates; D002800:Cholinesterase Inhibitors; D002091:Butyrylcholinesterase; D002118:Calcium
Farmakologicheskaia izbiratel'nost' ingibitorov kholinésteraz, obuslovlennaia ikh antagonizmom s ionami kal'tsiia.