Donepezil Hydrochloride (E2020) and Other Acetylcholinesterase Inhibitors
| Autor: | Youichi Iimura, Yoshiyuki Kawakami, Yoshiharu Yamanishi, Hachiro Sugimoto |
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| Rok vydání: | 2000 |
| Předmět: |
Models
Molecular Physostigmine medicine.drug_class Aché Pharmacology Crystallography X-Ray Biochemistry Structure-Activity Relationship chemistry.chemical_compound Piperidines Alzheimer Disease Donepezil Hydrochloride Drug Discovery medicine Animals Humans Donepezil Adverse effect business.industry Organic Chemistry Brain Stereoisomerism Acetylcholinesterase language.human_language Rats chemistry Acetylcholinesterase inhibitor Tacrine Indans language Molecular Medicine Cholinesterase Inhibitors business medicine.drug |
| Zdroj: | Current Medicinal Chemistry. 7:303-339 |
| ISSN: | 0929-8673 |
| DOI: | 10.2174/0929867003375191 |
| Popis: | A wide range of evidence shows that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, namely, physostigmine and tacrine, showed modest improvement in the cognitive function of Alzheimer's patients. However, clinical studies show that physostigmine has poor oral activity, brain penetration and pharmacokinetic parameters while tacrine has hepatotoxic liability. Studies were then focused on finding a new type of acetylcholinesterase inhibitor that would overcome the disadvantages of these two compounds. Donepezil hydrochloride inaugurates a new class of AChE inhibitors with longer and more selective action with manageable adverse effects. Currently, there are about 19 new Alzheimer's drugs in various phases of clinical development. |
| Databáze: | OpenAIRE |
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