Mini-Reviews in Medicinal Chemistry


Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS Activity and Treatment of Cognitive Dysfunction in Central Neurodegenerative Diseases

Author(s): Alan D. Borthwick.


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 disease

Keywords: Alzheimer's, depression, fluparoxan, schizophrenia, α2-adrenoceptor antagonist.

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Article Details

Year: 2017
Page: [572 - 582]
Pages: 11
DOI: 10.2174/1389557516666160321115041
Price: $58