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 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 language | English (US) |
---|---|
Pages (from-to) | 3732-3738 |
Number of pages | 7 |
Journal | Current pharmaceutical design |
Volume | 21 |
Issue number | 26 |
DOIs | |
State | Published - Sep 1 2015 |
Keywords
- 5-HT receptors
- 5-HTreceptors
- Antipsychotic drugs
- Atypical antipsychotic drugs
- Constitutive activity
- Inverse agonism
- Schizophrenia
- Serotonin
ASJC Scopus subject areas
- Drug Discovery
- Pharmacology