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Clozapine and Haloperidol Differentially Alter the Constitutive Activity of Central Serotonin2C Receptors In Vivo
| Content Provider | Semantic Scholar |
|---|---|
| Author | Navailles, Sylvia Deurwaerdère, Philippe De Spampinato, Umberto |
| Copyright Year | 2006 |
| Abstract | BACKGROUND Central serotonin2C (5-HT2C) receptors are known to play a role in the mechanism of action of the antipsychotic drugs (APDs) clozapine and haloperidol. However, evidence for the involvement of the constitutive activity of 5-HT2C receptors in the dopamine (DA)ergic effects of APDs is lacking in vivo. METHODS Using in vivo microdialysis in halothane-anesthetized rats, we assessed the ability of selective 5-HT2C compounds to modulate the release of DA induced by haloperidol and clozapine in the nucleus accumbens and striatum. RESULTS Both APDs induced a dose-dependent increase in accumbal and striatal DA extracellular levels. The effect of .01 mg/kg haloperidol was potentiated by the 5-HT2C inverse agonist SB 206553 (5 mg/kg) but unaltered by the 5-HT2C antagonists SB 243213 and SB 242084 (1 mg/kg). Conversely, the effect of 1 mg/kg clozapine, a dose able to reverse the decrease in DA outflow induced by the 5-HT2C agonist Ro 60-0175 (3 mg/kg), was unaffected by SB 206553 but blocked by SB 243213 (1 mg/kg) and SB 242084 (.3 and 1 mg/kg). CONCLUSIONS These results show that clozapine and haloperidol differentially alter the constitutive activity of 5-HT2C receptors and suggest that clozapine behaves as a 5-HT2C inverse agonist in vivo. |
| Starting Page | 568 |
| Ending Page | 575 |
| Page Count | 8 |
| File Format | PDF HTM / HTML |
| DOI | 10.1016/j.biopsych.2005.07.035 |
| Alternate Webpage(s) | https://api.elsevier.com/content/article/pii/S0006322305009248 |
| Alternate Webpage(s) | https://www.sciencedirect.com/science/article/pii/S0006322305009248?dgcid=api_sd_search-api-endpoint |
| PubMed reference number | 16182256 |
| Alternate Webpage(s) | https://doi.org/10.1016/j.biopsych.2005.07.035 |
| Journal | Medline |
| Volume Number | 59 |
| Journal | Biological Psychiatry |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
