Pharmacologic approaches that diminish dopamine-mediated neural transmission in brain have antipsychotic actions in humans. Blockade of D2 family dopamine receptors is the most common strategy. A paradoxical strategy of using dopamine agonists in particular circumstances to similarly diminish dopaminergic transmission is based on the known function of dopamine autoreceptors and on consideration of the intrinsic activity of dopamine agonists. It was apomorphine that first suggested the effectiveness of dopamine agonist treatment for schizophrenia. Now a partial dopamine agonist aripiprazole has come to market for psychosis and others are in development. This chapter reviews the clinical pharmacology of partial dopamine agonists and their development for the treatment of schizophrenia.
Keywords: affinity, intrinsic activity, apomorphine, n-propyl-noraporphine, 3ppp aripiprazole