Atypical antipsychotics and inverse agonism at 5-HT2 receptors

Laura C. Sullivan, William P. Clarke, Kelly A. Berg

Research output: Contribution to journalArticlepeer-review

32 Scopus citations


It is now well accepted that receptors can regulate cellular signaling pathways in the absence of a stimulating ligand, and inverse agonists can reduce this ligand-independent or “constitutive” receptor activity. Both the serotonin 5-HT2A and 5-HT2C receptors have demonstrated constitutive receptor activity in vitro and in vivo. Each has been identified as a target for the treatment of schizophrenia. Further, most, if not all, atypical antipsychotic drugs have inverse agonist properties at both 5-HT2A and 5-HT2C receptors. This paper describes our current knowledge of inverse agonism of atypical antipsychotics at 5-HT2A/2C receptor subtypes in vitro and in vivo. Exploiting inverse agonist properties of antipsychotic drugs may provide new avenues for drug development.

Original languageEnglish (US)
Pages (from-to)3732-3738
Number of pages7
JournalCurrent pharmaceutical design
Issue number26
StatePublished - Sep 1 2015


  • 5-HT receptors
  • 5-HTreceptors
  • Antipsychotic drugs
  • Atypical antipsychotic drugs
  • Constitutive activity
  • Inverse agonism
  • Schizophrenia
  • Serotonin

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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