Abstract
The inhibition of huperzine A, a potential therapeutic agent to treat Alzheimer's disease, on rat cortical acetylcholinesterase was found to be highly stereospecific. In the present study the effect of the enantiomers of huperzine A on [ 3H]dizocilpine (MK-801) binding to synaptic membrane of rat cerebral cortex was compared. The natural (−)-huperzine A and the synthetic (+)-huperzine A inhibited the specific binding of [ 3H]MK-801 with a similar potency. The IC 50 values were 65±7 and 82±12 μM ( n=5 for each enantiomer, P=0.248), respectively. The result indicates that huperzine A inhibits N-methyl- d-aspartate (NMDA) receptor in rat cerebral cortex without stereoselectivity.
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