SB-242,084

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SB-242,084
SB242084.png
Systematic (IUPAC) name
6-chloro-5-methyl-N-{6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl]indoline-1-carboxamide
Clinical data
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

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] In animal studies, SB-242,084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines.[10]

See also[edit]

References[edit]

  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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. 
  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. doi:10.1016/j.biopsych.2006.11.023. PMC 2129095. PMID 17524369. 
  10. ^ 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.  edit