SB-242084
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| CAS Number | 181632-25-7 |
| PubChem (CID) | 3644637 |
| IUPHAR/BPS | 193 |
| ChEMBL | CHEMBL14563 |
| Chemical and physical data | |
| Formula | C21H19ClN4O2 |
| Molar mass | 394.853 g/mol |
| 3D model (Jmol) | Interactive image |
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SB-242084 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] In animal studies, SB-242084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines.[10]
See also[edit]
References[edit]
- ^ 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. - ^ 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.
- ^ Manvich, D. F.; Kimmel, H. L.; Cooper, D. A.; Howell, L. L. (2012). "The Serotonin 2C Receptor Antagonist SB 242084 Exhibits Abuse-Related Effects Typical of Stimulants in Squirrel Monkeys". Journal of Pharmacology and Experimental Therapeutics. 342 (3): 761–9. doi:10.1124/jpet.112.195156. PMID 22685342.
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