CAS NO: | 120786-18-7 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
(±)-Huperzine A 是传统中草药中提取的活性石松属生物碱,是可逆的乙酰胆碱酯酶(ACE)抑制剂,在中国被广泛的运用于阿尔茨海默病。
Cas No. | 120786-18-7 |
别名 | (±)-石杉碱甲 |
化学名 | (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 |
分子式 | C15H18N2O |
分子量 | 242.32 |
溶解度 | DMSO : ≥ 50 mg/mL (206.34 mM) |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | (–)-Huperzine A (HupA) is an acetylcholinesterase (AChE) inhibitor with an IC50 value of 82 nmol/L [1] and acts as an antagonist of the N-methyl-d-aspartate (NMDA) receptor [2]. AChE is the key brain enzyme responsible for the rapid degradation of the neurotransmitter acetylcholine. AChE inhibitors are probably useful in the amelioration of the Alzheimer’s symptomatology [3]. It was found that NMDA markedly reduced AChE activities [4]. In rat dissociated hippocampal neurons, HupA inhibited the NMDA-induced current. In neurons, 100 μM HupA, NMDA-induced currents were 55.7 ± 4.9% of the control values. The binding molecular ratio of NMDA receptor: HupA is 1:1. The inhibition of NMDA receptor by HupA is not competitive [5]. HupA significantly increased the phosphorylation levels of both glycogen synthase kinase (GSK)-3α protein and GSK-3β protein in APPsw-overexpressing cells [2]. Activated GSK-3 consequently decreased acetylcholine (ACh) level in the striatum [6]. Treated with doses of (–)-huperzine A, AChE–/– mice showed no toxic symptoms and had normal levels of AChE. This demonstrated the specificity of (–)-huperzine A as an inhibitor of AChE at the dose used in vivo [7]. In rat whole brain, oral administration of HupA at a dose of 1.5 μmol/kg (3.6 mg/kg) obtained a maximum inhibition of AChE at 60 min and this maximum inhibition was maintained for 360 min [8]. References: |