Mechanism of action of cholinesterase inhibitors in Alzheimer's disease.
Cholinesterase inhibitors, such as physostigmine and tacrine, have lately gained interest as potential drugs in the treatment of Alzheimer's disease. Already in the 1950s, it was discovered that physostigmine and tacrine were potent inhibitors of acetylcholinesterase and butyrylcholinesterase. However, later studies have shown that cholinesterase inhibitors also interact with cholinergic receptors, with sodium and potassium ion channels and effect the uptake, synthesis and release of neurotransmitters. In summary, cholinesterase inhibitors are drugs with many modes of action, which may be of advantage in the treatment of a complex disorder such as Alzheimer's disease.
Håkansson
L
L
Department of Pharmaceutical Biosciences, Uppsala University, Sweden.
D000109:Acetylcholine / Q000378:metabolism; D000368:Aged; D000544:Alzheimer Disease / Q000188:drug therapy* / Q000201:enzymology / Q000503:physiopathology; D001921:Brain / Q000187:drug effects / Q000201:enzymology / Q000503:physiopathology; D002091:Butyrylcholinesterase / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D006801:Humans; D008297:Male; D018377:Neurotransmitter Agents / Q000378:metabolism; D010830:Physostigmine / Q000494:pharmacology* / Q000627:therapeutic use; D011950:Receptors, Cholinergic / Q000187:drug effects; D013619:Tacrine / Q000494:pharmacology* / Q000627:therapeutic use
D002800:Cholinesterase Inhibitors; D018377:Neurotransmitter Agents; D011950:Receptors, Cholinergic; D013619:Tacrine; D010830:Physostigmine; D002091:Butyrylcholinesterase; D000109:Acetylcholine