Huperzine A (HupA) is a sesquiterpene alkaloid derived from the fir-like moss Huperzia serrata; it exhibits anticonvulsant/antiepileptic, neuromodulatory, cognition enhancing, neuroprotective, and antinociceptive activities. HupA acts as a reversible, selective acetylcholinesterase (AChE) inhibitor and is being explored in clinical trials as a potential treatment for Alzheimer’s Disease. Several studies have shown HupA to improve cognition, memory, mood, and/or daily activities at a range of doses. Additionally, HupA’s comparatively long-lasting binding of AChE is protective against organophosphate-induced seizure and status epilepticus. In cellular and animal models, this compound exhibits non-competitive, reversible antagonist activity at NMDA receptors. HupA is also under examination as a potential non-dependence-inducing antinociceptive, as it blocks chemical, thermal, and mechanical pain stimulation in vivo.