Pharmacological Activity of Novel Anticholinesterase Agents of Potential Use in the Treatment of Alzheimer’s Disease
In dementia of the Alzheimer type there is a selective loss in the cerebral cortex of choline acetyltransferase (CAT), the enzyme that synthesizes acetylcholine (ACh)1,2. The degree of dementia and memory impairment that occurs in this condition is well correlated with the decrement in cortical cholinergic transmission3. Moreover, scopolamine, a cholinergic antagonist, can cause memory impairment in normal individuals similar to that in aging4. These findings suggest that impaired cortical cholinergic transmission may be at least in part responsible for the symptomatology of Alzheimer disease. In support of this suggestion it was found that physostigmine, which prevents the destruction of ACh, can cause memory improvement in Alzheimer patients5. The extent of improvement of the symptomatology was closely related to the degree of inhibition of acetylcholinesterase (AChE) in the spinal fluid, and thus to the amount of physostigmine reaching the central nervous system6.
KeywordsAChE Activity Corpus Striatum Brain AChE Phenyl Carbamate Choline Acetyl Transferase
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