Schizophrenia is characterised by positive, negative, cognitive, depressive and anxiety symptoms. Over the last decades a number of novel treatment strategies with better clinical efficacy and scope, but with lower side-effect profiles have been developed. These have significantly improved the management and prognosis of the disease. Of these approaches, modulation of the serotonergic receptor system is a common, recurring, theme; particularly the use of 5-HT1A receptor agonism as part of or adjunct to existing therapies. Here we review data exploring the utility of 5-HT1A receptor agonists for extending the actions of antipsychotic agents, while limiting their side-effect profile. Notably, interest has grown concerning 5-HT1A receptor activation in schizophrenia because of the development of novel antipsychotics, such as lurasidone and cariprazine, the characterisation of 5-HT1A receptor polymorphisms in schizophrenia patients and the possible beneficial influence of 5-HT1A agonists on neurogenesis.