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Huperzine A Introductions

Publish Date 2019-09-10
Melting Point: 217-219 degrees Celcius

Molar Mass: 242.32 g/mol

Molecular Formula: C15H18N2O

Huperzine A is naturally occurring. It is an alkaloid compound found in the firmoss Huperzia Serrata.

Firmoss Huperzia Serrata is a plant which is widely distributed over the counter as a dietary supplement. It may treat Alzheimers Disease.

It is native to India and Southeast Asia.

The mechanism of action is similar to Donepezil, Rivastigmine, and Galantamine.

Huperzine A is commonly sold in the USA for memory support. The botanical itself has long been used by the Chinese to treat swelling, fever and blood disorders.

Clinical trials in China have proven the drug helps improve memory function and treats Alzheimers disease.

Being an acetylcholinesterase inhibitor and NMDA receptor antagonist, the drug is able to break down acetylcholine which will increase the level and duration of the neurotransmitter acetylcholine. Huperzine A is one of the only naturally occurring acetylcholinesterase inhibitors. Some of the major side effects may include: actions on the parasympathetic nervous system, may cause bradycardia (a resting heart rate), hypotension (abnormally low blood pressure), hypersecretion (releasing chemicals), bronchoconstriction (constriction of airways in the lungs due to the tightening of smooth muscle – shortness of breath and weezing / coughing may occur), GI tract hypermotility (diarrhea), and may decrease intraocular pressure (releasing pressure behind eyes). It may also cause SLUDGE syndrome (Salivation, Lacrimation, Urination, Defecation, Gastrointenstinal upset, Emesis - Vomitting). It may also cause actions on the neuromuscular junction, prolonging muscle contraction.

Brief Background

Huperzine A is an alkaloid isolated from Chinese club moss Huperzia serrata, a member of the Lycopodium family (1), developed by the Chinese Academy of Sciences (2). Teas and decoctions brewed from these primitive plants have traditionally been used in China for treatment of fever, inflammation, and swelling, as well as for a variety of psychological conditions, including mental illness, and as a memory aid. Huperzine As potential as a memory enhancer is the primary reason for the current widespread interest in its use both as a dietary supplement and as a unique pharmacotherapy for degenerative brain disorders, such as Alzheimers disease.

Considerable theoretical basis and bench scientific evidence supports huperzine As potential in reducing or even preventing certain kinds of neuronal dysfunction associated with learning and memory impairment, including Alzheimers disease and related conditions. Huperzine A may act by at least two distinct molecular mechanisms, both of which are consistent with its putative effects on enhancing memory and cognition: The first hypothesis suggests that huperzine A is a naturally occurring "slow" cholinesterase inhibitor that increases acetylcholine levels in the synapse and in peripheral tissues. The cholinergic hypothesis of Alzheimers disease implicates a reduced synthesis of acetylcholine; however, this hypothesis has not gained widespread support, mainly due to the inability of medications that treat acetylcholine deficiency to alleviate symptoms of Alzheimers (acetylcholine has been implicated since deficits in this neurotransmitter in the brain impair learning and cognition). The second main hypothesis is that huperzine A competitively inhibits N-methyl D-aspartate (NMDA) receptors in brain cells. NMDA receptors mediate glutamate, an excitatory amino acid; such modulation may result in neurotoxicity, which has been implicated in the causation and symptomatology of Alzheimers and other neurodegenerative conditions.

Huperzine A has shown promising results in the treatment of Alzheimers disease in early and relatively small randomized clinical trials. Phase II clinical trials in the United States (1) and phase III trials in China are underway to investigate the use of this agent for the treatment of Alzheimers disease

Based on its molecular modes of action and some in vivo evidence, huperzine A has promise as a neuroprotective agent against vascular (hypoxic or ischemic) brain injury in both the very young and the very old, and is also under active scrutiny as a pre-exposure agent for use in the event of organophosphate nerve gas attack. However, there is currently a lack of human data available for these indications.

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