In vivo kinetics of blood cholinesterase inhibition by 9-amino-1, 2, 3, 4-tetrahydroacridine, its 7-methoxy derivative and physostigmine in rats.
In vivo inhibition of blood acetylcholinesterase activity by 9-amino-1, 2, 3, 4-tetrahydroacridine, its 7-methoxy derivative and physostigmine was studied in rats. Changes of enzyme activity in the blood were continually registered using an automatic colorimeter Auto Analyzer system. The dependence of % enzyme inhibition upon time in semilogarithmic transformation was characterized by a two phase curve. The first phase reflected the increase in the concentration of inhibitors in the blood during their resorption; this was followed by a slow second phase of inhibition. The inhibitory effect decreased in the order: physostigmine greater than tacrine greater than 7-methoxytacrine. The relationship between the anticholinesterase and antipsychotomimetic action of the examined substances is discussed.
D000110:Acetylcholinesterase / Q000097:blood*; D000166:Acridines / Q000494:pharmacology*; D000818:Animals; D007700:Kinetics; D008297:Male; D010830:Physostigmine / Q000494:pharmacology*; D051381:Rats; D013619:Tacrine / Q000031:analogs & derivatives / Q000494:pharmacology*
D000166:Acridines; D013619:Tacrine; D010830:Physostigmine; D000110:Acetylcholinesterase