From Self-sufficiency
Jump to: navigation, search
Systematic (IUPAC) name
CAS Number 181632-25-7
PubChem CID 3644637
Chemical data
Formula C21H19ClN4O2
Molar mass 394.853 g/mol[[Script error: No such module "String".]]
Script error: No such module "collapsible list".
Script error: No such module "TemplatePar".Expression error: Unexpected < operator.

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]


Cite error: Invalid <references> tag; parameter "group" is allowed only.

Use <references />, or <references group="..." />
  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. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20. PMID 9225286
  2. Martin JR, Ballard TM, Higgins GA. Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety. Pharmacology, Biochemistry and Behaviour. 2002 Apr;71(4):615-25. PMID 11888553
  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. 1999 Aug;38(8):1195-205. PMID 10462132
  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. 2004 Feb;29(2):319-26. PMID 14560323
  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. 2006 Nov;99(4):1311-9. PMID 17018023
  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. 2008 Jan;33(2):237-46. PMID 17429406
  7. Leggio GM, Cathala A, Moison D, Cunningham KA, Piazza PV, Spampinato U. Serotonin(2C) receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens. Neuropharmacology. 2008 Oct 17. PMID 18977370
  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. Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade. Neuropsychopharmacology. 2004 Oct;29(10):1782-9. PMID 15138437
  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. 2007 Nov 15;62(10):1111-8. PMID 17524369