Studies on new,centrally active and reversible acetylcholinesterase inhibitors |
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| Authors: | Frank Arnal Lucien J. Coté Sara Ginsburg Glen D. Lawrence Ali Naini Mary Sano |
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| Affiliation: | (1) Department of Neurology, College of Physicians & Surgeons, Columbia University, 630 West 168th Street, 10032 New York, N.Y.;(2) Clremistry Deprtment, Long Island University, 11201 Brooklyn, New York;(3) Neurological Institute, 710 West 168th Street, 10032 New York, N.Y. |
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| Abstract: | We have synthesized the tertiary amines of pyridostigmine and neostigmine, 3-pyridinol dimethylcarbamate (norpyridostigmine) and 3-dimethylaminophenol dimethylcarbamate (norneostigmine) respectively, and we have tested their abilities to cross the blood-brain barrier and inhibit mouse brainAChE activity. The in vivo inhibition of AChE activity by norpyridostigmine reaches 72% at 10 minutes which is comparable to that seen with physostigmine (73% at 10 minutes). Inhibition by norneostigmine is less effective (50% at 10 minutes) and approaches that obtained with tetrahydroaminoacridine (57% at 10 minutes). These data show that both norpyridostigmine and norneostigmine cross the blood-brain barrier and that they are effective inhibitors of mouse brain AChE activity. These drugs could be useful in the treatment of memory, impairment associated with Alzheimer's disease, and other memory disorders. |
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| Keywords: | Acetylcholinesterase inhibitors physostigmine tetrahydroaminoacridine mouse brain |
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