Natural and synthetic Huperzine A: effect on cholinergic function in vitro and in vivo.
Huperzine A has been shown to be useful in the treatment of symptoms of dementia of the Alzheimer type. Our initial attempts to synthesize (-)Huperzine A resulted in the racemic mixture of (+/-)Huperzine A. We have therefore compared the in vitro and in vivo effects of (+/-)Huperzine A with those of (-)Huperzine A in rats. The results indicate a similar biological mechanism of action between the two, but that the racemic mixture of (+/-)Huperzine A has a weaker biological activity than the natural product (-)Huperzine A, presumably due to the presence in the mixture of (+)Huperzine A, which is considerably less potent than the (-)isomer.
Hanin
I
I
Department of Pharmacology and Experimental Therapeutics, Loyola University Chicago, Stritch School of Medicine, Maywood, Illinois 60153.
Tang
X C
XC
Kindel
G L
GL
Kozikowski
A P
AP
D000109:Acetylcholine / Q000378:metabolism; D000110:Acetylcholinesterase / Q000378:metabolism*; D000470:Alkaloids; D000544:Alzheimer Disease / Q000188:drug therapy; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D051381:Rats; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D013237:Stereoisomerism
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D012717:Sesquiterpenes; C050426:huperzine A; D000110:Acetylcholinesterase; D000109:Acetylcholine