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    HUPERZINE-A molecular structure

    HUPERZINE-A Stats & Data

    H-a
    NPS DataHub
    MW242.32
    FormulaC15H18N2O
    CAS102518-79-6
    IUPAC(1''R'',9''R'',13''E'')-1-Amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0²,⁷]trideca-2(7),3,10-trien-5-one
    SMILESCC=C1C2C=C(C)CC1(N)c1ccc(=O)nc1C2
    InChIKeyZRJBHWIHUMBLCN-YQEJDHNASA-N
    Chemical Class Lycopodium alkaloid

    Pharmacology

    DrugBank
    State Solid

    Description

    Huperzine A, is a naturally occurring sesquiterpene alkaloid found in the extracts of the firmoss _Huperzia serrata_. The botanical has been used in China for centuries 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.

    Mechanism of Action

    Huperzine A has been found to be an inhibitor of the enzyme acetylcholinesterase. This is the same mechanism of action of pharmaceutical drugs such as galantamine and donepezil used to treat Alzheimer's disease.

    Pharmacodynamics

    Huperzine A is an alkaloid derived from <i>Huperzia serrata</i> (which is available as an herbal product in the US). It is under investigation as an acetylcholinesterase inhibitor. Clinical trials in China have shown that huperzine A is comparably effective to the drugs currently on the market, and may even be somewhat safer in terms of side effects.

    Indication

    Investigated for use/treatment in alzheimer's disease.

    Measured Affinities

    Guide to PHARMACOLOGY

    Measured binding and functional data for huperzine A, curated by the IUPHAR/BPS Guide to PHARMACOLOGY. Each row cites the paper it came from. Lower concentrations mean tighter binding — a value in the sub-nanomolar range indicates a very potent interaction.

    Target Action Measure Value Concentration Species Source
    acetylcholinesterase (Yt blood group) ACHE Inhibition pKd 7.77 16.98 nM Human PMID 33570950

    Reading this. pKi, pEC50 and pIC50 are negative log molar values, so a higher number means a tighter interaction; the concentration column converts them for you. Values from non-human species are laboratory measurements and do not translate directly to human effect. Receptor affinity is not a dose — it describes what a molecule binds, not how much of it is safe to take.

    Receptor data from the IUPHAR/BPS Guide to PHARMACOLOGY (v2026.2), licensed CC BY-SA 4.0. Matched to this substance by InChIKey.

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