Laura C. Sullivan, William P Clarke and Kelly A. Berg Pages 3732 - 3738 ( 7 )
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-HT<sub>2A</sub> and 5-HT<sub>2C</sub> 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-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptors. This paper describes our current knowledge of inverse agonism of atypical antipsychotics at 5-HT<sub>2A/2C</sub> receptor subtypes <i>in vitro</i> and <i>in vivo</i>. Exploiting inverse agonist properties of APDs may provide new avenues for drug development.
Antipsychotic drugs, atypical antipsychotic drugs, inverse agonism, constitutive activity, serotonin, 5-HT<sub>2A</sub> receptors, 5-HT<sub>2C</sub> receptors, schizophrenia.
, , Department of Pharmacology – MS 7764, University of Texas Health Science Center, 7703 Floyd Curl Drive, San Antonio, TX 78229-3900, USA.