Galanthamine HBr

2 years -80 in solvent

S.c. twice a day or 3 or 6 hours after ischemia and at subsequent 12-hours intervals until sacrifice

Galanthamine is now under the phase IV clinical trials for the efficacy and safety for improving dysfunction in people with bipolar disorder.

Galanthamine is dissolved in 0.9% NaCl saline solution.

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 uM) 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 uM) activates single-channel currents in outside-out patches excised from clonal PC12 cells. [3]

Acetylcholinesterase Assay, The catalytic activity of acetylcholinesterase in erythrocytes and brain is measured using [14C]acetylcholine iodide radiolabelled in the acetyl moiety at a final substrate concentration of 3.6 mmM, a pH of 7.4 and a temperature of 25 C. Concentration response trials are then performed. After incubation of the sample with Galanthamine for 60 minutes at 25 C in vitro, the catalytic reaction is started by the addition of substrate.

Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.