Accession NumberDB05510
TypeSmall Molecule

Huperzine-A is a naturally occurring sesquiterpene alkaloid found in the extracts of the firmoss Huperzia serrata. The botanical has traditionally been used in China for the treatment of swelling, fever and blood disorders. Recently in clinical trials in China, it has demonstrated neuroprotective effects. It is currently being investigated as a possible treatment for diseases characterized by neurodegeneration, particularly Alzheimer’s disease. Huperzine A is a cholinesterase inhibitor.

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Investigated for use/treatment in alzheimer's disease.

Structured Indications Not Available

Huperzine A is a cholinesterase inhibitor. This is the same mechanism of action of pharmaceutical drugs such as galantamine and donepezil used to treat Alzheimer's disease. There is evidence that huperzine A may compare favorably in symptomatic efficacy to cholinesterase inhibitors currently in use. In addition, huperzine A has antioxidant and neuroprotective properties that suggest that it may be useful as a disease-modifying treatment for Alzheimer's disease (AD). The drug is currently available as a nutraceutical in this country, and is being used by some U.S. clinicians to treat AD. However, there have been no controlled clinical trials outside China assessing its toxicity and efficacy.

Mechanism of action

As a quasi-irreversible inhibitor of acetylcholinesterase, Huperzine A is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine.

TargetKindPharmacological actionActionsOrganismUniProt ID
AcetylcholinesteraseProteinunknownNot AvailableHumanP22303 details
Related Articles
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General References
  1. Little JT, Walsh S, Aisen PS: An update on huperzine A as a treatment for Alzheimer's disease. Expert Opin Investig Drugs. 2008 Feb;17(2):209-15. doi: 10.1517/13543784.17.2.209. [PubMed:18230054 ]
  2. Li WM, Kan KK, Carlier PR, Pang YP, Han YF: East meets West in the search for Alzheimer's therapeutics - novel dimeric inhibitors from tacrine and huperzine A. Curr Alzheimer Res. 2007 Sep;4(4):386-96. [PubMed:17908041 ]
  3. Haviv H, Wong DM, Silman I, Sussman JL: Bivalent ligands derived from Huperzine A as acetylcholinesterase inhibitors. Curr Top Med Chem. 2007;7(4):375-87. [PubMed:17305579 ]
  4. Akhondzadeh S, Abbasi SH: Herbal medicine in the treatment of Alzheimer's disease. Am J Alzheimers Dis Other Demen. 2006 Mar-Apr;21(2):113-8. [PubMed:16634467 ]
  5. Wang R, Yan H, Tang XC: Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine. Acta Pharmacol Sin. 2006 Jan;27(1):1-26. [PubMed:16364207 ]
  6. Wang R, Tang XC: Neuroprotective effects of huperzine A. A natural cholinesterase inhibitor for the treatment of Alzheimer's disease. Neurosignals. 2005;14(1-2):71-82. [PubMed:15956816 ]
  7. Authors unspecified: Huperzine A. Drugs R D. 2004;5(1):44-5. [PubMed:14725492 ]
  8. Jiang H, Luo X, Bai D: Progress in clinical, pharmacological, chemical and structural biological studies of huperzine A: a drug of traditional chinese medicine origin for the treatment of Alzheimer's disease. Curr Med Chem. 2003 Nov;10(21):2231-52. [PubMed:14529340 ]
  9. Zangara A: The psychopharmacology of huperzine A: an alkaloid with cognitive enhancing and neuroprotective properties of interest in the treatment of Alzheimer's disease. Pharmacol Biochem Behav. 2003 Jun;75(3):675-86. [PubMed:12895686 ]
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Clinical Trials
Clinical Trials
4Unknown StatusTreatmentDementias / Schizophrenic Disorders1
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Spectrum TypeDescriptionSplash Key
ClassificationNot classified


Pharmacological action
General Function:
Serine hydrolase activity
Specific Function:
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
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Molecular Weight:
67795.525 Da
Drug created on November 18, 2007 11:25 / Updated on August 17, 2016 12:24