期刊
CURRENT PHARMACEUTICAL DESIGN
卷 21, 期 26, 页码 3732-3738出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1381612821666150605111236
关键词
Antipsychotic drugs; atypical antipsychotic drugs; inverse agonism; constitutive activity; serotonin; 5-HT2A receptors; 5-HT2C receptors; schizophrenia
资金
- Janssen Scientific Affairs, LLC
- National Institutes of Health, USPHS [T32DA031115]
- NATIONAL INSTITUTE ON DRUG ABUSE [T32DA031115] Funding Source: NIH RePORTER
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.
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