Partial agonism and schizophrenia

Recent literature on partial agonists has Recent literature on partial agonists has generated interest in their therapeutic generated interest in their therapeutic potential in schizophrenia. This has been potential in schizophrenia. This has been driven, in part, by the recent approval of driven, in part, by the recent approval of the dopamine (D2) receptor partial agonist the dopamine (D2) receptor partial agonist aripiprazole in the USA and Europe. In aripiprazole in the USA and Europe. In comparison with conventional and atypical comparison with conventional and atypical antipsychotics that mediate their therapeu-antipsychotics that mediate their therapeutic effects by D2 receptor blockade, aripi-tic effects by D2 receptor blockade, aripiprazole has a unique mechanism of action. prazole has a unique mechanism of action. However, the concept of partial agonists However, the concept of partial agonists for the treatment of schizophrenia is not for the treatment of schizophrenia is not entirely novel, since aripiprazole is one of entirely novel, since aripiprazole is one of several members of this class of drug. This several members of this class of drug. This editorial reviews the neurochemistry of editorial reviews the neurochemistry of dopamine in schizophrenia and discusses dopamine in schizophrenia and discusses the theoretical importance of partial agon-the theoretical importance of partial agonism as a mechanism for the treatment of ism as a mechanism for the treatment of this illness. We also summarise the histori-this illness. We also summarise the historical information on previous trials of partial cal information on previous trials of partial agonists in schizophrenia and evaluate agonists in schizophrenia and evaluate other dopamine receptor partial agonists other dopamine receptor partial agonists that are currently under development. that are currently under development.