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Huperzine A
Billy Boy
Posted: Thursday, October 17, 2013 10:33 AM
Joined: 4/16/2012
Posts: 5

Has anyone tried Huperzine A? It looks interesting when you google it.
Posted: Friday, October 18, 2013 10:43 PM
Joined: 10/16/2013
Posts: 2

Looks hopeful!  I'm going to check into it!
Posted: Friday, October 18, 2013 10:57 PM
Joined: 12/6/2011
Posts: 3326

Huperzine A

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Huperzine A Identifiers CAS number 102518-79-6 N ChemSpider 16736021 YesY DrugBank DB01928 ChEMBL CHEMBL395280 YesY Jmol-3D images Image 1 Properties Molecular formula C15H18N2O Molar mass 242.32 g/mol Melting point

217–219 °C

N (verify) (what is: YesY/N?)
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) Infobox references

Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata.[1] and in varying quantities in other Huperzia species, including H. elmeri, H. carinat, and H. aqualupian.[2]

Huperzine A is also an acetylcholinesterase inhibitor, which has a mechanism of action similar to donepezil, rivastigmine, and galantamine. A pro-drug form of huperzine A (ZT-1) is under development as a treatment for Alzheimer's disease.[3]

In the US, huperzine A is sold as a dietary supplement for memory support. The botanical has been used in China for centuries for the treatment of swelling, fever and blood disorders. Clinical trials in China have shown it to be effective in improving cognitive performance in patients with Alzheimer's disease[4] and enhancing memory in adolescents complaining of memory inadequacy.[5]

Pharmacological effects[edit]

Huperzine A is an acetylcholinesterase inhibititor[6] and NMDA receptor antagonist.[7]

Huperzine A has also attracted the attention of US medical science. It is currently being investigated as a possible treatment for diseases characterized by neurodegeneration – particularly Alzheimer's disease.[8][9] It has been found to be an inhibitor of the enzyme acetylcholinesterase.[10] The structure of the complex of huperzine A with acetylcholinesterase has been determined[11] by X-ray crystallography (PDB code: 1VOT; see the 3D structure). This is the same mechanism of action of pharmaceutical drugs such as galantamine and donepezil used to treat Alzheimer's disease. Huperzine A is also a NMDA receptor antagonist which may either reduce or increase glutamate induced damage in brain and increase nerve growth factor levels in rats.[12]

Clinical trials in China have shown that huperzine A is comparably effective to similar drugs on the market, and may even be safer in terms of side effects.[4] The National Institute on Aging has completed[9] a Phase II clinical trial[13] to evaluate the safety and efficacy of huperzine A in the treatment of Alzheimer's disease in a randomized controlled trial of its effect on cognitive function. In 2008, the National Institute on Aging conducted the first controlled trial outside of China evaluating the efficacy and toxicity of huperzine A to improve cognitive function in patients with AD. In this multi-center, double-blind, placebo-controlled Phase II trial, 210 participants with mild to moderate AD received either 200 mcg of huperzine A, 400 mcg of huperzine A, or placebo twice daily for 16 weeks. While no statistical difference in cognitive scores was noted in patients in the lower dose huperzine A group compared to placebo, the higher dose (400 mcg) of huperzine A led to improved cognition and activities of daily living. However, no significant changes were noted in any of the three groups in overall change in disease or in psychiatric ratings according to the AD Assessment Scale-Cognitive (ADAS-Cog) scale. Huperzine A was safe and well tolerated in the study. (13)

The same year, a Cochrane Database review examined studies evaluating the efficacy and safety of huperzine A in the treatment of AD. The review included six randomized, controlled trials involving 454 patients. The conclusion was that the currently available evidence is insufficient to assess the potential for huperzine A in the treatment of MCI. Randomised double-blind placebo-controlled trials are needed.[14]

Possible side effects include[citation needed] breathing problems, tightness in the throat or chest, chest pain, skin hives, rash, itchy or swollen skin, upset stomach, diarrhea, vomiting, hyperactivity and insomnia. Most adverse events were cholinergic in nature and no serious adverse events occurred. Huperzine A is a well-tolerated drug.[6]