Anticholinesterase effects of huperzine A, E2020, and tacrine in rats.
OBJECTIVE
To compare the anticholinesterase effects of huperzine A (Hup A), E2020, and tacrine in rats.


METHODS
Spectrophotometry was used to determine AChE activity in brain and BuChE activity in serum.


RESULTS
Following intragastric gavage, Hup A, E2020, and tacrine all produced dose-dependent inhibitions of brain AChE. Oral Hup A exhibited a higher inhibition than E2020 and tacrine. Tacrine was more effective in inhibiting serum BuChE correlated with severe peripheral adverse effects. The BuChE activity was less affected by Hup A and E2020. After a single oral dose of Hup A, a relatively steady state of AChE inhibition produced, which was longer than that after E2020 and tacrine. No change in the cholinesterase inhibition was seen for the 3 drugs following repeated i.g. medications.


CONCLUSIONS
Hup A i.g. exhibited a higher efficacy, a longer duration of action, and a more selective inhibition on AChE than E2020 and tacrine.
Wang
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State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Tang
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XC
D000110:Acetylcholinesterase / Q000378:metabolism; D000470:Alkaloids; D000818:Animals; D001921:Brain / Q000201:enzymology; D002091:Butyrylcholinesterase / Q000097:blood; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D000077265:Donepezil; D004305:Dose-Response Relationship, Drug; D005260:Female; D066298:In Vitro Techniques; D007189:Indans / Q000494:pharmacology*; D008297:Male; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012717:Sesquiterpenes / Q000494:pharmacology*; D013619:Tacrine / Q000494:pharmacology*
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D007189:Indans; D010880:Piperidines; D012717:Sesquiterpenes; C050426:huperzine A; D013619:Tacrine; D000077265:Donepezil; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase