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SB-242,084: Wikis

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SB-242,084
Systematic (IUPAC) name
6-chloro-5-methyl-N-{6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl]indoline-1-carboxamide
Identifiers
CAS number 181632-25-7
ATC code  ?
PubChem 3644637
Chemical data
Formula C 21H19ClN4O2  
Mol. mass 394.853 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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]

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. 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
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