Atypical antipsychotics and inverse agonism at 5-HT2 receptors

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

Journal Name: Current Pharmaceutical Design

Volume 21 , Issue 26 , 2015

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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.

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Article Details

VOLUME: 21
ISSUE: 26
Year: 2015
Page: [3732 - 3738]
Pages: 7
DOI: 10.2174/1381612821666150605111236
Price: $65

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