Galanthaminone是竞争性可逆的胆碱酯酶（AChE）抑制剂，可作用于多种记忆障碍疾病。
Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments. AChE
Galanthaminone reduces the action of AChE and therefore tends to increase the concentration of acetylcholine in the brain. is also an allosteric ligand at nicotinic acetylcholine receptors. It has shown activity in modulating the nicotinic cholinergic receptors on cholinergic neurons to increase acetylcholine release.
Absorption of Galanthaminone is rapid and complete and shows linear pharmacokinetics. It is well absorbed with absolute oral bioavailability between 80 and 100%. It has a half-life of seven hours. Peak effect of inhibiting acetylcholinesterase was achieved about one hour after a single oral dose of 8 mg in some healthy volunteers.
[1]. Greenblatt HM, et al. Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 1999 Dec 17;463(3):321-6. [2]. Heinrich M, et al. Galanthamine from snowdrop--the development of a modern drug against Alzheimer's disease from local Caucasian knowledge. J Ethnopharmacol. 2004 Jun;92(2-3):147-62.
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