Galantamine (hydrobromide) (Synonyms: Galanthamine, NSC 100058)

Galantamine is an alkaloid that has been found in Galanthus and has acetylcholinesterase (AChE) inhibitory and nicotinic acetylcholine receptor (nAChR) potentiating activities.^1,2,3 It selectively inhibits AChE over butyrylcholinesterase (BChE; IC₅₀s = 636 and 8,404 nM, respectively).² Galantamine (0.5 µM) potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs. In vivo, galantamine (1.3 mg/kg per day) decreases escape latency and path length in the Morris water maze in the APP23 transgenic mouse model of Alzheimer’s disease.⁴ Formulations containing galantamine have been used in the treatment of Alzheimer’s disease.

1.Harvey, A.L.The pharmacology of galanthamine and its analoguesPharmacol. Ther.68(1)113-128(1995) 2.Rook, Y., Schmidtke, K.U., Gaube, F., et al.Bivalent β-carbolines as potential multitarget anti-Alzheimer agentsJ. Med. Chem.53(9)3611-3617(2010) 3.Samochocki, M., Zerlin, M., Jostock, R., et al.Galantamine is an allosterically potentiating ligand of the human α4/β2 nAChRActa Neurol. Scand. Suppl.17668-73(2000) 4.Van Dam, D., and De Deyn, P.P.Cognitive evaluation of disease-modifying efficacy of galantamine and memantine in the APP23 modelEur. Neuropsychopharmacol.16(1)59-69(2006)