SB-242,084
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| Systematic (IUPAC) name | |
| 6-chloro-5-methyl-N-{6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl]indoline-1-carboxamide | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 181632-25-7 |
| ATC code | ? |
| PubChem | CID 3644637 |
| IUPHAR ligand | 193 |
| ChEMBL | CHEMBL14563 |
| Chemical data | |
| Formula | C21H19ClN4O2 |
| Mol. mass | 394.853 g/mol |
| SMILES | eMolecules & PubChem |
SB-242,084 is a psychoactive drug and research chemical which acts as a selective antagonist for the 5HT2C receptor.[1] It has anxiolytic effects,[2] and enhances dopamine signalling in the limbic system,[3] as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions[4][5] but reducing it in others.[6][7] It has been shown to increase the effectiveness of the selective serotonin reuptake inhibitor (SSRI) class of antidepressants, and may also reduce their side effects.[8][9]
[edit] References
- ^ Kennett, GA; Wood, MD; Bright, F; Trail, B; Riley, G; Holland, V; Avenell, KY; Stean, T et al. (1997). "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist". Neuropharmacology 36 (4–5): 609–20. doi:10.1016/S0028-3908(97)00038-5. PMID 9225286.
- ^ Martin, JR; Ballard, TM; Higgins, GA (2002). "Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety". Pharmacology, biochemistry, and behavior 71 (4): 615–25. doi:10.1016/S0091-3057(01)00713-4. PMID 11888553.
- ^ Di Matteo, V; Di Giovanni, G; Di Mascio, M; Esposito, E (1999). "SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system". Neuropharmacology 38 (8): 1195–205. doi:10.1016/S0028-3908(99)00047-7. PMID 10462132.
- ^ Navailles, S; De Deurwaerdère, P; Porras, G; Spampinato, U (2004). "In vivo evidence that 5-HT2C receptor antagonist but not agonist modulates cocaine-induced dopamine outflow in the rat nucleus accumbens and striatum". Neuropsychopharmacology 29 (2): 319–26. doi:10.1038/sj.npp.1300329. PMID 14560323.
- ^ Navailles, S; Moison, D; Ryczko, D; Spampinato, U (2006). "Region-dependent regulation of mesoaccumbens dopamine neurons in vivo by the constitutive activity of central serotonin2C receptors". Journal of neurochemistry 99 (4): 1311–9. doi:10.1111/j.1471-4159.2006.04188.x. PMID 17018023.
- ^ Navailles, S; Moison, D; Cunningham, KA; Spampinato, U (2008). "Differential regulation of the mesoaccumbens dopamine circuit by serotonin2C receptors in the ventral tegmental area and the nucleus accumbens: an in vivo microdialysis study with cocaine". Neuropsychopharmacology 33 (2): 237–46. doi:10.1038/sj.npp.1301414. PMID 17429406.
- ^ Leggio, GM; Cathala, A; Moison, D; Cunningham, KA; Piazza, PV; Spampinato, U (2009). "Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens". Neuropharmacology 56 (2): 507–13. doi:10.1016/j.neuropharm.2008.10.005. PMC 3130963. PMID 18977370. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=3130963.
- ^ Cremers, TI; Giorgetti, M; Bosker, FJ; Hogg, S; Arnt, J; Mørk, A; Honig, G; Bøgesø, KP et al. (2004). "Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade". Neuropsychopharmacology 29 (10): 1782–9. doi:10.1038/sj.npp.1300474. PMID 15138437.
- ^ Burghardt, NS; Bush, DE; McEwen, BS; Ledoux, JE (2007). "Acute SSRIs Increase Conditioned Fear Expression: Blockade with a 5-HT2C Receptor Antagonist". Biological Psychiatry 62 (10): 1111–8. doi:10.1016/j.biopsych.2006.11.023. PMC 2129095. PMID 17524369. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2129095.
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