Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS activity and treatment of Cognitive Dysfunction in central Neurodegenerative diseases.

Background: The design, medicinal chemistry, pharmacokinetics and development of the highly selective alpha(2)-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 alpha(2)-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