Abstract
Background: The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed.
Method: The drug's activity and selectivity in vitro, its efficacy in animals and its excellent oral pharmacokinetics and central α2-adrenoceptor antagonist activity in man, are evaluated as well as its ability to increase extracellular levels of noradrenaline, dopamine and acetylcholine in vivo. Conclusion: Furthermore, its potential for the treatment of central neurodegenerative diseases is highlighted, in particular its improvement of cognitive dysfunction in schizophrenia and in models of Alzheimer's diseaseKeywords: Alzheimer's, depression, fluparoxan, schizophrenia, α2-adrenoceptor antagonist.
Mini-Reviews in Medicinal Chemistry
Title:Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS Activity and Treatment of Cognitive Dysfunction in Central Neurodegenerative Diseases
Volume: 17 Issue: 7
Author(s): Alan D. Borthwick*
Affiliation:
- DrugMolDesign, 15 Temple Grove, London NW11 7UA,United Kingdom
Keywords: Alzheimer's, depression, fluparoxan, schizophrenia, α2-adrenoceptor antagonist.
Abstract: Background: The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed.
Method: The drug's activity and selectivity in vitro, its efficacy in animals and its excellent oral pharmacokinetics and central α2-adrenoceptor antagonist activity in man, are evaluated as well as its ability to increase extracellular levels of noradrenaline, dopamine and acetylcholine in vivo. Conclusion: Furthermore, its potential for the treatment of central neurodegenerative diseases is highlighted, in particular its improvement of cognitive dysfunction in schizophrenia and in models of Alzheimer's diseaseExport Options
About this article
Cite this article as:
Borthwick D. Alan*, Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS Activity and Treatment of Cognitive Dysfunction in Central Neurodegenerative Diseases, Mini-Reviews in Medicinal Chemistry 2017; 17 (7) . https://dx.doi.org/10.2174/1389557516666160321115041
DOI https://dx.doi.org/10.2174/1389557516666160321115041 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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