Home Neuronal Signaling AChR inhibitor - GluR (-)-Huperzine A (HupA)

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(-)-Huperzine A (HupA) AChR inhibitor

Cat.No.S2251

(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.
(-)-Huperzine A (HupA) AChR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 242.32

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Quality Control

Batch: S225101 5%TFA]7.54 mg/mL]false]DMSO]Insoluble]false]Water]Insoluble]false Purity: 98.19%
98.19

Chemical Information, Storage & Stability

Molecular Weight 242.32 Formula

C15H18N2O

 Storage (From the date of receipt)
CAS No. 102518-79-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC=C1C2CC3=C(C1(CC(=C2)C)N)C=CC(=O)N3

Solubility

In vitro
Batch:

5%TFA : 7.54 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Features
Greater penetration of the blood-brain barrier, higher oral bioavailability, and longer AChE inhibition relative to tacrine, donepezil, and rivastigmine.
Targets/IC50/Ki
AChE (G4 form) [1]
7 nM(Ki)
In vitro
(-)-Huperzine A is a novel alkaloid isolated from the Chinese herb Huperzia serrata. (-)-Huperzine A preferentially inhibits tetrameric AChE (G4 form). (-)-Huperzine A is more potent than tacrine, physostigmine, galanthamine, and rivastigmine with respect to inhibition of AChE activity, whereas HupA is the least potent BuChE inhibitor among the inhibitors. [1] (-)-Huperzine A possesses the ability to protect cells against hydrogen peroxide, β-amyloid protein, glutamate, ischemia and staurosporine-induced cytotoxicity and apoptosis. These protective effects are related to its ability to attenuate oxidative stress, regulate the expression of apoptotic proteins Bcl-2, Bax, P53, and caspase-3, protect mitochondria, upregulate nerve growth factor and its receptors, and interfere with amyloid precursor protein metabolism. [3]
In vivo
(-)-Huperzine A can ameliorate the learning and memory deficiency in animal models and AD patients. Its potentially beneficial actions include modification of β-amyloid peptide processing, reduction of oxidative stress, neuronal protection against apoptosis, and regulation of the expression and secretion of nerve growth factor (NGF) and NGF signaling. [2] (-)-Huperzine A significantly inhibits AChE activity in the cortex, hippocampus, striatum, medial septum, medulla oblongata, cerebellum, and hypothalamus of rats that are killed 30 min following the administration of (-)-Huperzine A at several dose levels compared with the saline control. [3]
References

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