Galanthamine hydrobromide

• Catalog No.: S1339
• CAS Number: 1953-04-4
• M. F.: C17H22BrNO3
• M. W.: 368.26548
• Storage: -20°C

SYNONYMS

• IUPAC name: (1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.0^{1,12}.0^{6,17}]heptadeca-6,8,10(17),15-tetraen-14-ol hydrobromide
• IUPAC Traditional name: galantamine hydrobromide
• Synonyms: Reminyl

DATABASE IDS

• CAS Number: 1953-04-4

PROPERTIES

• Target: mAChRs mAChRs
• Salt Data: Hydrobromide
• Storage Condition: -20°C

DETAILS

Description (English)

Research Area

• Description: Neurological Disease

Biological Activity

• Description: Galanthamine (Razadyne, Reminyl) is an AChE inhibitor with IC50 of 14 nM.
• Targets: AChE
• IC50: 14 nM ^[1]
• In Vitro: 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]
• 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. ^[4]
• Clinical Trials: Galanthamine is now under the phase IV clinical trials for the efficacy and safety for improving dysfunction in people with bipolar disorder.

Protocol

• Protocol: Kinase Assay ^[1]
• 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.
• Protocol: Animal Study ^[4]
• Animal Models: Gerbils
• Formulation: Galanthamine is dissolved in 0.9% NaCl saline solution.
• Doses: 10 mg/kg
• Administration: S.c. twice a day or 3 or 6 hours after ischemia and at subsequent 12-hours intervals until sacrifice

References

• References: [1] Thomsen T, et al. Eur J Clin Chem Clin Biochem, 1991, 29(8), 487-492.
• References: [2] Pereira EF, et al. J Pharmacol Exp Ther, 1994, 270(2), 768-778.
• References: [3] Storch A, et al. Eur J Pharmacol, 1995, 290(3), 207-219.
• References: [4] Lorrio S, et al. J Pharmacol Exp Ther, 2007, 322(2), 591-599.

REFERENCES

• Thomsen T, et al. Eur J Clin Chem Clin Biochem, 1991, 29(8), 487-492.
• Pereira EF, et al. J Pharmacol Exp Ther, 1994, 270(2), 768-778.
• Storch A, et al. Eur J Pharmacol, 1995, 290(3), 207-219.
• Lorrio S, et al. J Pharmacol Exp Ther, 2007, 322(2), 591-599.