Pacheco_1995_J.Pharmacol.Exp.Ther_274_767

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Title : Cholinesterase inhibitors proposed for treating dementia in Alzheimer's disease: selectivity toward human brain acetylcholinesterase compared with butyrylcholinesterase - Pacheco_1995_J.Pharmacol.Exp.Ther_274_767
Author(s) : Pacheco G , Palacios-Esquivel R , Moss DE
Ref : Journal of Pharmacology & Experimental Therapeutics , 274 :767 , 1995
Abstract : One consistent finding in senile dementia of the Alzheimer's type is that the brain has reduced ability to synthesize acetylcholine. This has been related, in part, to memory dysfunctions. Although a cholinergic deficit is not singularly responsible for symptoms of dementia, treatment strategies have been designed to facilitate cholinergic activity by inhibiting acetylcholinesterase (AChE). To minimize toxicity, however, a cholinesterase inhibitor selective for only AChE would be an ideal treatment. The purpose of this study was to determine the selectivity of physostigmine, metrifonate, methanesulfonyl fluoride and tetrahydroaminoacridine (tacrine) toward AChE as compared with butyrylcholinesterase (BChE) in human cortex. The results show that methanesulfonyl fluoride is selective as an inhibitor of AChE as compared with BChE. Physostigmine inhibited AChE more than BChE. Metrifonate was found to inhibit BChE more than AChE. Tetrahydroaminoacridine inhibited both enzymes in a complex way.
ESTHER : Pacheco_1995_J.Pharmacol.Exp.Ther_274_767
PubMedSearch : Pacheco_1995_J.Pharmacol.Exp.Ther_274_767
PubMedID: 7636741

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Pacheco G, Palacios-Esquivel R, Moss DE (1995)
Cholinesterase inhibitors proposed for treating dementia in Alzheimer's disease: selectivity toward human brain acetylcholinesterase compared with butyrylcholinesterase
Journal of Pharmacology & Experimental Therapeutics 274 :767

Pacheco G, Palacios-Esquivel R, Moss DE (1995)
Journal of Pharmacology & Experimental Therapeutics 274 :767