Galanthamine hydrobromide 是一种长效的中枢活性 AChE 抑制剂,IC50为 410 nM。它是神经元烟碱型 ACh 受体的变构增强剂,IC50值为 0.35 μM,可用于阿尔茨海默症的研究。
产品描述
Galanthamine hydrobromide, a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.
体外活性
Galanthamine has been demonstrated to have an IC50 of 14 nM and 15 nM on AChE in post-mortem human brain frontal cortex and the hippocampus region. Red-cell cholinesterase activity in blood samples from the neurosurgery patients is 10 times more strongly inhibited by Galanthamine in brain tissue samples. [1] Galanthamine (1 μM) activates single channels with conductance's of 18 and 30 pS in outside-out patches excised from dexamethasone mouse fibroblasts (M10 cells). [2] Galanthamine acts as noncompetitive nicotinic receptor agonists' on clonal rat pheochromocytoma (PC12) cells. Galanthamine (50 μM) activates single-channel currents in outside-out patches excised from clonal PC12 cells. [3]
体内活性
Galantamine significantly increases the number of living pyramidal neurons after ischemia-reperfusion injury. Galantamine significantly reduces TUNEL, active caspase-3, and SOD-2 immunoreactivity. The nicotinic antagonist mecamylamine blockes the protective effects of galantamine. The neuroprotective effects of galantamine are preserved even when first administered at 3 hours postischemia. [4]
Cas No.
1953-04-4
分子式
C17H22BrNO3
分子量
368.271
别名
Galanthamine HBr;氢溴酸加兰他敏;Galantamine hydrobromide
储存和溶解度
H2O:7.4 mg/mL (20 mM)
DMSO:7.4 mg/mL (20 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years