| Description | Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors. |
| In vitro | Galanthamine hydrobromide 对人脑前额皮层和海马区的乙酰胆碱酯酶(AChE)的IC50 值为 14 nM和15 nM。此外，神经外科患者血液样本中的红细胞胆碱酯酶活性被Galanthamine hydrobromide 抑制的程度是脑组织样本中的10倍。[1]Galanthamine hydrobromide (1 μM) 可激活从Dexamethasone acetate小鼠成纤维细胞（M10 细胞）中切除的外向斑块中电导为 18 和 30 pS 的单通道。[2]在克隆大鼠嗜铬细胞瘤(PC12)细胞上，Galanthamine hydrobromide 是克隆大鼠嗜铬细胞瘤（PC12）细胞上的非竞争性烟碱受体激动剂。Galanthamine hydrobromide（50 μM）可激活从克隆 PC12 细胞中切除的外切斑块的单通道电流。[3] |
| In vivo | Galanthamine hydrobromide 显著提高了缺血-再灌注损伤后存活的锥体神经元数量。Galanthamine hydrobromide 显著降低TUNEL标记、活化的caspase-3 活化的以及SOD-2免疫反应。尼古丁拮抗剂美卡明阻断了Galanthamine hydrobromide 的保护作用。即使在缺血后3小时给药，Galanthamine hydrobromide 的神经保护效应仍然存在。[4] |
| Target activity | AChE:410 nM |
| Synonyms | Galantamine hydrobromide, Galanthamine HBr, 氢溴酸加兰他敏 |
| molecular weight | 368.27 |
| Molecular formula | C17H21NO3·HBr |
| CAS | 1953-04-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (162.92 mM), Heating is recommended. H2O: 7.4 mg/mL (20 mM) |
| References | 1. Thomsen T, et al. Eur J Clin Chem Clin Biochem, 1991, 29(8), 487-492. 2. Pereira EF, et al. J Pharmacol Exp Ther, 1994, 270(2), 768-778. 3. Storch A, et al. Eur J Pharmacol, 1995, 290(3), 207-219. 4. Lorrio S, et al. J Pharmacol Exp Ther, 2007, 322(2), 591-599. |