Partial agonism of dopamine, serotonin and opiate receptors for psychiatry

Most psychiatric diseases are treated with pharmacological receptor antagonists. The efficacy of recently approved partial agonists and their relatively good safety profiles suggest an alternative strategy for drug discovery. Aripiprazole (Abilify) treats schizophrenia through partial agonism of D2/3 dopamine receptors, buspirone (Buspar) treats anxiety or depression by partial agonism of the 5-HT1A receptor and partial opiate or dopamine agonists treat opiate and stimulant addictions. Predictions of other receptor targets for intervention by partial agonists provide a test for the broader utility of this pharmacological approach.

Section editors:David Sibley – National Institute of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, USAC. Anthony Altar – Psychiatric Genomics, Gaithersburg, USATheresa Branchek – Lundbeck Research, Paramus, USA