Anabasine derivatives as reversible and irreversible inhibitors of cholinesterases from different animals

A comparative study was carried out of action of 18 specifically synthesized anabasine derivatives and their analogs, including diiodomethylates of anabasine acylates and bis-anabasine derivatives of dicarboxylic glutaric, adipic, azelaic, and sebacic acids, on activity of cholinesterase of brain of frog Rana temporaria and visual ganglia of the Pacific squid Todarodes pacificus and Commander squid Berryteuthis magister from different zones of habitations in the northwest part of the Pacific Ocean as well as of erythrocyte acetylcholinesterase and serum butyrylcholinesterase. These compounds were not submitted to cholinesterase hydrolysis and turned out to be efficient reversible inhibitors that have to certain degree specificity toward the studied enzymes both by their potency and by the type of their inhibitory action. Specificity of effects of the key structural fragments of the anabasine grouping on anticholinesterase efficacy was checked. Also performed was analysis of action of 24 reversible and irreversible organophosphorus inhibitors, anabasine derivatives, toward erythrocyte acetylcholinesterase and serum butyrylcholinesterase. The anticholinesterase effects of anabasine-containing inhibitors differing in structure and action mechanism was compared.