Studies on new, centrally active and reversible acetylcholinesterase inhibitors
| Autor: | Frank Arnal, Lucien J. Cote, Sara Ginsburg, Glen D. Lawrence, Ali Naini, Mary Sano |
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| Rok vydání: | 1990 |
| Předmět: |
Male
Physostigmine Aché Dopamine Pharmacology Blood–brain barrier Biochemistry Cellular and Molecular Neuroscience chemistry.chemical_compound Mice Norepinephrine In vivo medicine Animals biology Chemistry Brain General Medicine Acetylcholinesterase language.human_language Neostigmine medicine.anatomical_structure Pyridostigmine Enzyme inhibitor Blood-Brain Barrier language biology.protein Tacrine Cholinesterase Inhibitors medicine.drug Pyridostigmine Bromide |
| Zdroj: | Neurochemical research. 15(6) |
| ISSN: | 0364-3190 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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