GPR139 agonist-2 (compound 20a) is a potent GPR139 agonist with an EC 50 of 24.7 nM. GPR139 agonist-2 rescues the social interaction deficits and alleviates cognitive deficits in murine schizophrenia models. GPR139 agonist-2 has the potential for antischizophrenia drug research.