(-)-Huperzine A

(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC₅₀ of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease^{[1][2][3][4][5]}. IC50 & Target:IC50: 82 nM (AChE) ^[1], NMDA^[3] In Vitro:(-)-Huperzine A (1 μM; 2 hours) attenuates Aβ23-35 (20 μM)-induced neuronal injury^[2].
(-)-Huperzine A (100 μM) reversibly inhibits the NMDA-induced current (IC₅₀=126 μM) in whole-cell voltage-clamp recording in CA1 pyramidal neurons acutely dissociated from rat hippocampus^[3].
In Vivo:(-)-Huperzine A (0.1-0.2 mg/kg; i.p.; daily; for 12 days) can alleviate the cognitive dysfunction and neuronal degeneration induced by i.c.v. infusion of beta-amyloid protein-(1-40) in rats^[5].