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