Serotonin 5-HT1A Receptors and Antipsychotics - An Update in Light of New Concepts and Drugs

Curr Pharm Des. 2015;21(26):3725-31. doi: 10.2174/1381612821666150605105215.


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.

Publication types

  • Review

MeSH terms

  • Antipsychotic Agents / pharmacology*
  • Antipsychotic Agents / therapeutic use
  • Humans
  • Mood Disorders / drug therapy
  • Mood Disorders / physiopathology
  • Receptor, Serotonin, 5-HT1A / drug effects*
  • Receptor, Serotonin, 5-HT1A / physiology
  • Schizophrenia / drug therapy
  • Schizophrenia / physiopathology
  • Serotonergic Neurons / drug effects
  • Serotonergic Neurons / physiology


  • Antipsychotic Agents
  • Receptor, Serotonin, 5-HT1A