The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure

The identification of a highly selective D2 partial agonist, D3 antagonist tool molecule which demonstrates high levels of brain exposure and selectivity against an extensive range of dopamine, serotonin, adrenergic, histamine, and muscarinic receptors is described.

The identification of a hitherto unprecedented pharmacology in a compound (3) displaying highly selective DA D2 partial agonism and DA D3 antagonism, but devoid of activity at other aminergic receptors is described.Figure optionsDownload as PowerPoint slide