Galanthamine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Galanthamine是乙酰胆碱酯酶(AChE)的有效抑制剂,其IC50值为410 nM[1]。
乙酰胆碱酯酶是一种水解酶,属于羧酸酯酶家族。其能水解神经递质乙酰胆碱,并具有较高的催化活性。AChE存在于多种传导组织:神经、肌肉、运动和感觉纤维以及中枢和外周组织。AChE位于突触后膜。其通过水解ACh抑制信号传递。ACh在神经传递中起重要作用。ACh释放到突触间隙,之后与位于突触后膜的ACh受体结合。抑制AChE的活性会使ACh积累在突触后膜,从而阻碍神经传递。AChE也是老年痴呆症的重要靶点[1]。
在SH-SY5Y细胞中,Galanthamine能显著抑制300 nM毒胡萝卜素诱导的细胞凋亡。在LDH试验中,10 nM Galanthamine能显著提高神经母细胞瘤的细胞活力。300 nM Galanthamine也能提高Aβ处理的细胞活力。300 nM Galanthamine能将嗜铬细胞中Bcl-2的表达水平提高3.1倍[1]。
3 mg/kg Galanthamine处理能显著提高小鼠海马体中IGF2的mRNA和蛋白水平。Galanthamine也能短暂降低BDNF mRNA水平,提高FGF2 mRNA水平[2]。
参考文献:
[1]. Arias E, Ales E, Gabilan NH, Cano-Abad MF, Villarroya M, Garcia AG, Lopez MG: Galantamine prevents apoptosis induced by beta-amyloid and thapsigargin: involvement of nicotinic acetylcholine receptors. Neuropharmacology 2004, 46(1):103-114.
[2]. Kita Y, Ago Y, Takano E, Fukada A, Takuma K, Matsuda T: Galantamine increases hippocampal insulin-like growth factor 2 expression via alpha7 nicotinic acetylcholine receptors in mice. Psychopharmacology (Berl), 225(3):543-551.
2. Liu Y, Zhang Y, et al. "Galantamine improves cognition, hippocampal inflammation, and synaptic plasticity impairments induced by lipopolysaccharide in mice." J Neuroinflammation. 2018 Apr 18;15(1):112. PMID:29669582
Storage | Store at -20°C |
M.Wt | 287.35 |
Cas No. | 357-70-0 |
Formula | C17H21NO3 |
Solubility | ≥14.37 mg/mL in DMSO; ≥14.43 mg/mL in H2O with gentle warming; ≥45 mg/mL in EtOH with gentle warming |
Chemical Name | (4aS,6R,8aS)-3-methoxy-11-methyl-5,6,9,10,11,12-hexahydro-4aH-benzo[2,3]benzofuro[4,3-cd]azepin-6-ol |
SDF | Download SDF |
Canonical SMILES | [H][C@@]([C@@]1(C([H])=C2[H])C3=C(C([H])=C4[H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])(C([H])([H])[C@@]2([H])O[H])OC3=C4OC([H])([H])[H] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1-3]: | |
细胞系 |
验尸人脑额叶皮层和海马区,M10细胞,大鼠嗜铬细胞瘤(PC12)细胞 |
溶解方法 |
可溶于DMSO。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
0.35 μM |
Applications |
在验尸人脑额叶皮层和海马区域中,Galanthamine抑制AChE的乙酰胆碱酯酶活性,IC50分别为14 nM和15 nM。在来自神经外科手术患者的血液样品中的红细胞中,Galanthamine对脑组织样品中的胆碱酯酶活性具有10倍更强的抑制。在从地塞米松小鼠成纤维细胞(M10细胞)的外膜上,Galanthamine(1 μM)激活单通道。在克隆大鼠的嗜铬细胞瘤(PC12)细胞中,Galanthamine作为非竞争性烟碱受体激动剂。Galanthamine(50 μM)激活克隆PC12细胞外膜上的单通道电流。 |
动物实验 [4]: | |
动物模型 |
雄性ddY小鼠 |
给药剂量 |
腹腔注射,0.3-3 mg/kg |
应用 |
腹腔内快速给药0.3-3 mg/kg Galantamine以时间和剂量依赖的方式增加IGF2 mRNA水平。腹腔注射3 mg/kg剂量的Galantamine增加了海马中的成纤维细胞生长因子2的mRNA水平,降低脑源性神经营养因子mRNA水平。Galantamin增加海马IGF2蛋白。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Thomsen T, Kaden B, Fischer J P, et al. Inhibition of acetylcholinesterase activity in human brain tissue and erythrocytes by galanthamine, physostigmine and tacrine[J]. Clinical Chemistry and Laboratory Medicine, 1991, 29(8): 487-492. [2]. Pereira E F, Alkondon M, Reinhardt S, et al. Physostigmine and galanthamine: probes for a novel binding site on the alpha 4 beta 2 subtype of neuronal nicotinic acetylcholine receptors stably expressed in fibroblast cells[J]. Journal of Pharmacology and Experimental Therapeutics, 1994, 270(2): 768-778. [3]. Storch A, Schrattenholz A, Cooper J C, et al. Physostigmine, galanthamine and codeine act as ‘noncompetitive nicotinic receptor agonists’ on clonal rat pheochromocytoma cells[J]. European Journal of Pharmacology: Molecular Pharmacology, 1995, 290(3): 207-219. [4]. Kita Y, Ago Y, Takano E, et al. Galantamine increases hippocampal insulin-like growth factor 2 expression via α7 nicotinic acetylcholine receptors in mice[J]. Psychopharmacology, 2013, 225(3): 543-551. |
Description | Galanthamine是AChE的抑制剂,IC50值为0.35 μM。 | |||||
靶点 | AChE | |||||
IC50 | 0.35 μM |
质量控制和MSDS
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