Chemistry:SB-242084

From HandWiki
Short description: Chemical compound
SB-242084
SB242084.png
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC21H19ClN4O2
Molar mass394.86 g·mol−1
3D model (JSmol)

SB-242084 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-242084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines.[10]

See also

References

  1. ↑ "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist". Neuropharmacology 36 (4–5): 609–20. 1997. doi:10.1016/S0028-3908(97)00038-5. PMID 9225286. 
  2. ↑ "Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety". Pharmacology, Biochemistry, and Behavior 71 (4): 615–25. April 2002. doi:10.1016/S0091-3057(01)00713-4. PMID 11888553. 
  3. ↑ "SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system". Neuropharmacology 38 (8): 1195–205. August 1999. doi:10.1016/S0028-3908(99)00047-7. PMID 10462132. 
  4. ↑ "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. doi:10.1038/sj.npp.1300329. PMID 14560323. 
  5. ↑ "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. doi:10.1111/j.1471-4159.2006.04188.x. PMID 17018023. 
  6. ↑ "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. doi:10.1038/sj.npp.1301414. PMID 17429406. 
  7. ↑ "Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens". Neuropharmacology 56 (2): 507–13. February 2009. doi:10.1016/j.neuropharm.2008.10.005. PMID 18977370. 
  8. ↑ "Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade". Neuropsychopharmacology 29 (10): 1782–9. October 2004. doi:10.1038/sj.npp.1300474. PMID 15138437. 
  9. ↑ "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. doi:10.1016/j.biopsych.2006.11.023. PMID 17524369. 
  10. ↑ "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. doi:10.1124/jpet.112.195156. PMID 22685342. 



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