Generic placeholder image

Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Atypical antipsychotics and inverse agonism at 5-HT2 receptors

Author(s): Laura C. Sullivan, William P Clarke and Kelly A. Berg

Volume 21, Issue 26, 2015

Page: [3732 - 3738] Pages: 7

DOI: 10.2174/1381612821666150605111236

Price: $65

Abstract

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 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 APDs may provide new avenues for drug development.

Keywords: Antipsychotic drugs, atypical antipsychotic drugs, inverse agonism, constitutive activity, serotonin, 5-HT2A receptors, 5-HT2C receptors, schizophrenia.


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy