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 disease