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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Neuronal Signal Pathway > GalanthamineCAS：357-70-0
Molecular Formula：C17H21NO3
Molecular Weight：287.35
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 357-70-0 |
| Name | Galanthamine |
| Molecular Formula | C17H21NO3 |
| Molecular Weight | 287.35 |
| Solubility | Soluble in Water/DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 609-175-3 |
| MDL | MFCD00867189 |
| SMILES | O[C@@H]1C[C@@H]2OC3=C4C(CN(C)CC[C@]42C=C1)=CC=C3OC |
| InChIKey | ASUTZQLVASHGKV-JDFRZJQESA-N |
| InChI | InChI=1S/C17H21NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19H,7-10H2,1-2H3/t12-,14-,17-/m0/s1 |
| PubChem CID | 9651 |
| Target Point | AChE |
| Passage | Neuronal Signaling |
| Background | Galanthamine is a potent acetylcholinesterase (AChE) inhibitor. |
| Biological Activity | Galanthamine 是一种有效的乙酰胆碱酯酶 (AChE) 抑制剂，IC50 为 500 nM。[1-3] |
| IC50 | 0.5μM(AChE)[1] |
| In Vitro | 加兰他敏抑制AChE和BChE，IC50为0.5和8.5μM[1]。加兰他敏充当在永久转染的HEK 293细胞中表达的人α4β2AChR的正变构调节剂(PAM)。加兰他敏使(α4β2)2α5AChRs对1μMACh的响应增加高达220％，浓度非常低(EC50 = 0.25 nM)。使用FLEXstation测定仅检测到α4β2或(α4β2)2β3AChR的小增强(20％)。浓度为1μM及以上的加兰他敏可抑制所有三种AChR亚型[2]。 |
| In Vivo | 加兰他敏(0.3-3mg/kg，ip)的急性给药以时间和剂量依赖性方式增加海马中的IGF2 mRNA水平，但不增加前额皮质中的IGF2 mRNA水平。加兰他敏(3 mg/kg，ip)引起海马中成纤维细胞生长因子2 mRNA水平的瞬时增加和脑源性神经营养因子mRNA水平的降低，而它不影响其他神经营养因子/生长因子的mRNA水平。加拉他敏诱导的海马IGF2 mRNA水平的增加被非选择性烟碱乙酰胆碱(ACh)受体(nAChR)拮抗剂Mecamylamine和选择性α7nAChR拮抗剂Methyllycaconitine阻断，但不受Telenzepine，一种优先的M1muscarinic ACh受体拮抗剂的阻断。此外，选择性α7nAChR激动剂PHA-543613增加IGF2 mRNA水平，而乙酰胆碱酯酶抑制剂Donepezil则不增加。加兰他敏还可以增加海马IGF2蛋白，后者被Methyllycaconitine阻断[2]。 |
| Animal Experiment | 小鼠[2]在受控环境条件下(22±1°C; 12：12-h)，将8周龄雄性ddY小鼠圈养在笼中(24 cm×17 cm×12 cm)，每组5至6只动物。在实验中使用之前，在实验时使用光暗周期，在0800小时开灯，食物和水随意放置1周。总共使用453只小鼠，并且一次性用于各种目的。使用以下药物：美卡拉明，甲基乌头碱，氧代震颤素和西仑西平，以及加兰他敏，多奈哌齐和PHA-543613。将所有药物溶解在盐水(0.9％NaCl溶液)中。药物以10mL/kg的体积腹膜内(ip)(加兰他敏，多奈哌齐，美卡拉明，甲基甘氨酸，氧代震颤素)或皮下(sc)(PHA-543613，Telenzepine)给药。 |
| Data Literature Source | [1]. Melanie-Jayne R. Howes，et al. Acetylcholinesterase inhibitors of natural origin. International Journal of Research in Pharmaceutical and Biomedical Sciences 3(SI 1):67-86. [2]. Kuryatov A，et al. Roles of accessory subunits in alpha4beta2(*) nicotinic receptors. Mol Pharmacol. 2008 Jul;74(1):132-43. [3]. Kita Y，et al. Galantamine increases hippocampal insulin-like growth factor 2 expression via α7 nicotinic acetylcholine receptors in mice. Psychopharmacology (Berl). 2013 Feb;225(3):543-51. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 20mg |
是一种有效的乙酰胆碱酯酶 (AChE) 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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