Home Neuronal Signaling AChR inhibitor - GluR (-)-Huperzine A (HupA) For research use only.

(-)-Huperzine A (HupA)

(-)-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) Chemical Structure

(-)-Huperzine A (HupA) Chemical Structure

CAS: 102518-79-6

Selleck's (-)-Huperzine A (HupA) has been cited by 1 publication

Purity & Quality Control

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

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Signaling Pathway

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Biological Activity

Description (-)-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.
Features Greater penetration of the blood-brain barrier, higher oral bioavailability, and longer AChE inhibition relative to tacrine, donepezil, and rivastigmine.
Targets
AChE (G4 form) [1]
7 nM(Ki)
In vitro
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
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]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 0.1 mg/kg
Administration Orally

Chemical Information & Solubility

Molecular Weight 242.32 Formula

C15H18N2O
CAS No. 102518-79-6 SDF Download (-)-Huperzine A (HupA) SDF
Smiles CC=C1C2CC3=C(C1(CC(=C2)C)N)C=CC(=O)N3
Storage (From the date of receipt)

In vitro
Batch:

5%TFA : 7.54 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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