|Systematic (IUPAC) name|
|Mol. mass||394.853 g/mol|
SB-242,084 is a psychoactive drug and research chemical which acts as a selective antagonist for the 5HT2C receptor. It has anxiolytic effects, and enhances dopamine signalling in the limbic system, as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions but reducing it in others. 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. In animal studies, SB-242,084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.