SB-242084 explained

SB-242084 is a psychoactive drug and research chemical which acts as a selective antagonist for the 5HT_2C 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

• CEPC
• RS-102221
• SB-243213

Notes and References

1. Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S, Forbes IT, Brown AM, Middlemiss DN, Blackburn TP . 6 . SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist . Neuropharmacology . 36 . 4–5 . 609–20 . 1997 . 9225286 . 10.1016/S0028-3908(97)00038-5 . 23032157 .
2. Martin JR, Ballard TM, Higgins GA . Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety . Pharmacology, Biochemistry, and Behavior . 71 . 4 . 615–25 . April 2002 . 11888553 . 10.1016/S0091-3057(01)00713-4 . 19142495 .
3. Di Matteo V, Di Giovanni G, Di Mascio M, Esposito E . SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system . Neuropharmacology . 38 . 8 . 1195–205 . August 1999 . 10462132 . 10.1016/S0028-3908(99)00047-7 . 39658512 .
4. Navailles S, De Deurwaerdère P, Porras G, Spampinato U . 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 . February 2004 . 14560323 . 10.1038/sj.npp.1300329 . free .
5. Navailles S, Moison D, Ryczko D, Spampinato U . Region-dependent regulation of mesoaccumbens dopamine neurons in vivo by the constitutive activity of central serotonin2C receptors . Journal of Neurochemistry . 99 . 4 . 1311–9 . November 2006 . 17018023 . 10.1111/j.1471-4159.2006.04188.x . 43833462 .
6. Navailles S, Moison D, Cunningham KA, Spampinato U . 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 . January 2008 . 17429406 . 10.1038/sj.npp.1301414 . free .
7. Leggio GM, Cathala A, Moison D, Cunningham KA, Piazza PV, Spampinato U . Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens . Neuropharmacology . 56 . 2 . 507–13 . February 2009 . 18977370 . 3130963 . 10.1016/j.neuropharm.2008.10.005 .
8. Cremers TI, Giorgetti M, Bosker FJ, Hogg S, Arnt J, Mørk A, Honig G, Bøgesø KP, Westerink BH, den Boer H, Wikstrom HV, Tecott LH . 6 . Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade . Neuropsychopharmacology . 29 . 10 . 1782–9 . October 2004 . 15138437 . 10.1038/sj.npp.1300474 . free .
9. Burghardt NS, Bush DE, McEwen BS, LeDoux JE . Acute selective serotonin reuptake inhibitors increase conditioned fear expression: blockade with a 5-HT(2C) receptor antagonist . Biological Psychiatry . 62 . 10 . 1111–8 . November 2007 . 17524369 . 2129095 . 10.1016/j.biopsych.2006.11.023 .
10. Manvich DF, Kimmel HL, Cooper DA, Howell LL . The serotonin 2C receptor antagonist SB 242084 exhibits abuse-related effects typical of stimulants in squirrel monkeys . The Journal of Pharmacology and Experimental Therapeutics . 342 . 3 . 761–9 . September 2012 . 22685342 . 3422522 . 10.1124/jpet.112.195156 .