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)