Abstract
Huperzine A, a novel cholinesterase inhibitor, was found to inhibit the N-methyl- d-aspartate (NMDA) receptors in the brain. In this study, the mechanisms of the NMDA receptor inhibition were investigated using [ 3H]dizocilpine (MK-801) binding in synaptic membrane of rat cerebral cortex. Changing the concentrations of l-glutamate and l-glycine did not alter the potency of huperzine A. Spermidine caused rightward shift of the concentration–response curve of huperzine A, and considerably increased its IC 50 value. Huperzine A did not affect the potency of unlabeled (+)-MK-801 in [ 3H]MK-801 binding. Saturation binding studies reveal that huperzine A exerts a negative allosteric modulation on the MK-801 binding site within the NMDA receptor-channel. The results suggest that huperzine A is a non-competitive antagonist of the NMDA receptors, acting at one of the polyamine binding sites.
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