There are currently no effective therapeutics to treat cognitive impairments associated with schizophrenia (CIAS), which includes major deficits in attention, learning and memory. This thesis aimed to validate the use of GPR52 agonists, a novel class of drug, in the treatment of CIAS. Concomitantly, we established a more translation-focused approach to preclinical drug discovery and development for CIAS. Using our innovative, translation-focused approach, we demonstrated the pro-cognitive and antipsychotic effects of established and novel GPR52 agonists. We hope our findings contribute to the development of new therapies actually capable of addressing CIAS in patients.