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.
Current Pharmaceutical Design
Title:Atypical antipsychotics and inverse agonism at 5-HT2 receptors
Volume: 21 Issue: 26
Author(s): Laura C. Sullivan, William P Clarke and Kelly A. Berg
Affiliation:
Keywords: Antipsychotic drugs, atypical antipsychotic drugs, inverse agonism, constitutive activity, serotonin, 5-HT2A receptors, 5-HT2C receptors, schizophrenia.
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.
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Cite this article as:
Sullivan C. Laura, Clarke P William and Berg A. Kelly, Atypical antipsychotics and inverse agonism at 5-HT2 receptors, Current Pharmaceutical Design 2015; 21 (26) . https://dx.doi.org/10.2174/1381612821666150605111236
DOI https://dx.doi.org/10.2174/1381612821666150605111236 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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