| In Vitro | In vitro activity: 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. 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). 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. |
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| In Vivo | 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. |
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| Animal model | Gerbils |
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| Formulation & Dosage | Dissolved in 0.9% NaCl saline solution; 10 mg/kg; s.c. injection |
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| References | Eur J Clin Chem Clin Biochem. 1991 Aug;29(8):487-92; J Pharmacol Exp Ther. 2007 Aug;322(2):591-9. |
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