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(±)-Huperzine A (Synonyms: Hup A, (-)-Selagine)

カタログ番号GC11965

神経保護作用のあるAChE阻害剤

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(±)-Huperzine A 化学構造

Cas No.: 120786-18-7

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10mM (in 1mL DMSO)
$55.00
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5mg
$50.00
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10mg
$80.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

(?)-フペルジンA(HupA)は、アセチルコリンエステラーゼ(AChE)阻害剤であり、IC50値は82 nmol / L [1]であり、N-メチル-d-アスパラギン酸(NMDA)受容体の拮抗薬として作用します[2]。

AChEは、神経伝達物質アセチルコリンの迅速な分解に責任を持つ主要な脳酵素です。AChE阻害剤は、アルツハイマー症状の改善において有用である可能性があります[3]。

NMDAは、AChE活性を著しく低下させることがわかった[4]。ラットの分離された海馬ニューロンでは、HupAはNMDA誘発電流を抑制した。ニューロンでは、100?MのHupAにおいて、NMDA誘発電流はコントロール値の55.7±4.9%であった。NMDA受容体:HupAの結合分子比率は1:1であり、HupAによるNMDA受容体の阻害は競争的ではない[5]。 Hup A は APPsw過剰発現細胞内でグリコーゲンシンターゼキナーゼ(GSK)-3αタンパク質およびGSK-3βタンパク質の両方のリン酸化レベルを有意に増加させました[2]。活性化された GSK-3 によりストライアタム内でアセチルコリン( ACh )レベルが低下しました [6] 。

(?)-フペルジンAの投与量で処理されたAChE?/?マウスは、毒性症状を示さず、正常なAChEレベルを有していました。これにより、(?)-フペルジンAがin vivoで使用される用量において、AChEの阻害剤としての特異性が証明されました[7]。ラット全脳では、1.5μmol/kg(3.6mg/kg)のHupAを経口投与することで60分間に最大限度のAChE抑制が得られ、この最大限度は360分間維持されました[8]。

References:
[1].? MA Xiao-Chao, XIN Jian, WANG Hai-Xue, et al. Acute effects of huperzine A and tacrine on rat liver. Acta Pharmacol ogica Sinica, 2003, 24(3):247-250.
[2].? Zhong Ming Qian and Ya Ke. Huperzine A: is it an effective disease-modifying drug for Alzheimer's disease? Frontiers in Aging Neuroscience, 2014, 6:216.
[3].? V. Rajendran, Suo-Bao Rong, Ashima Saxena, et al. Synthesis of a hybrid analog of the acetylcholinesterase inhibitors huperzine A and huperzine B. Tetrahedron Letters, 2001, 42: 5359-5361.
[4].? J. R. Delfs, D. M. Saroff, Y. Nishida, et al. Effects of NMDA and its antagonists on ventral horn cholinergic neurons in organotypic roller tube spinal cord cultures. J. Neural Transm., 1997, 104(1):31-51.
[5].? J. M. Zhang and G. Y. Hu. Huperzine A, a nootropic alkaloid, inhibits N-methyl-D-aspartate-induced current in rat dissociated hippocampal neurons. Neuroscience, 2001, 105(3):663-9.
[6].? L. Zhao, C. B. Chu, J. F. Li, et al. Glycogen synthase kinase-3 reduces acetylcholine level in striatum via disturbing cellular distribution of choline acetyltransferase in cholinergic interneurons in rats. Neuroscience, 2013, 255:203-11.
[7].? Ellen G. Duysen, Bin Li, Sultan Darvesh, et al. Sensitivity of butyrylcholinesterase knockout mice to (?)-huperzine A and donepezil suggests humans with butyrylcholinesterase deficiency may not tolerate these Alzheimer's disease drugs and indicates butyrylcholinesterase function in neurotransmission. Toxicology, 2007, 233:60-69.
[8].? Rui Wang, Han Yan and Xi-can Tang. Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine. Acta Pharmacologica Sinica, 2006, 27:1-26.

Chemical Properties

Cas No. 120786-18-7 SDF
同義語 Hup A, (-)-Selagine
Chemical Name (5R,9R,E)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1H)-one
Canonical SMILES C/C=C1[C@@]2(N)C3=C(NC(C=C3)=O)C[C@]/1([H])C=C(C)C2
Formula C15H18N2O M.Wt 242.32
溶解度 DMSO : ≥ 50 mg/mL (206.34 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.1268 mL 20.6339 mL 41.2677 mL
5 mM 0.8254 mL 4.1268 mL 8.2535 mL
10 mM 0.4127 mL 2.0634 mL 4.1268 mL
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