About: SB-243213 is a research topic. Over the lifetime, 12 publications have been published within this topic receiving 616 citations. The topic is also known as: SB-243,213 & SB-243213.
TL;DR: In rats and rodents, SB-243213 may possess an improved anxiolytic profile compared to benzodiazepines, and also modulates dopaminergic transmission, lacks pro-psychotic properties and may have utility in the treatment of schizophrenia and motor disorders.
TL;DR: It is concluded that selective activation of 5-HT(2C) receptors stimulates GABA-ergic function in the SNr, and the clinical relevance of these data is discussed.
TL;DR: It is demonstrated that both VTA and NAc 5‐HT2CRs participate in the inhibitory control exerted by 5-HT2 CRs on accumbal DA release, and that the NAc shell may represent a primary action site for the CA of 5‐ HT2CRS.
Abstract: Central serotonin2C receptors (5-HT(2C)Rs) control the mesoaccumbens dopamine (DA) pathway. This control involves the constitutive activity (CA) of 5-HT(2C)Rs, and is thought to engage regionally distinct populations of 5-HT(2C)Rs, leading to opposite functional effects. Here, using in vivo microdialysis in halothane-anesthetized rats, we investigated the relative contribution of ventral tegmental area (VTA) and nucleus accumbens shell (NAc) 5-HT(2C)Rs in the phasic/tonic control of accumbal DA release, to specifically identify the nature (inhibition/excitation) of the control, and the role of the 5-HT(2C)R CA. Intra-VTA injections of the selective 5-HT(2C)R antagonists SB 242084 and/or SB 243213 (0.1-0.5 microg/0.2 microL) prevented the decrease in accumbal DA outflow induced by the 5-HT(2C)R agonist Ro 60-0175 (3 mg/kg, i.p), but did not affect the increase in DA outflow induced by the 5-HT(2C)R inverse agonist SB 206553 (5 mg/kg, i.p). Intra-NAc infusions of SB 242084 (0.1-1 microM) blocked Ro 60-0175- and SB 206553-induced changes of DA outflow. Intra-NAc, but not intra-VTA administration of SB 206553 increased basal DA outflow. These findings demonstrate that both VTA and NAc 5-HT(2C)Rs participate in the inhibitory control exerted by 5-HT(2C)Rs on accumbal DA release, and that the NAc shell may represent a primary action site for the CA of 5-HT(2C)Rs.
TL;DR: Results show that clozapine and haloperidol differentially alter the constitutive activity of 5-HT2C receptors and suggest that clozoapine behaves as a 5- HT2C inverse agonist in vivo.