What is it about?
The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed. 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. 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.
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Why is it important?
This is a comprehensive review of all the biological activity of Fluparoxan in animals and man as well as its design and synthesis
Perspectives
Fluparoxan is arguably the best of the very selective α2-adrenoceptor antagonists, it has been shown to possess central α2-adrenoceptor antagonist activity after both single and repeated oral doses in man with excellent bioavailability (97%) and a long duration of action (6-7hrs).
Consultant ALAN DAVID BORTHWICK
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This page is a summary of: 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, April 2017, Bentham Science Publishers,
DOI: 10.2174/1389557516666160321115041.
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