SB-242084

The importance of SB-242084 in today's society is unquestionable. Whether in the professional, personal or social sphere, SB-242084 occupies a relevant place in our lives. As the world evolves and technology advances, SB-242084 becomes increasingly indispensable, significantly impacting the way we interact and relate to others. In this article, we will explore the relevance of SB-242084 in various contexts and its influence on people's daily lives. From its origin to its impact today, we will analyze how SB-242084 has become a key element in our society.
SB-242084
Identifiers
  • 6-chloro-5-methyl-N-{6-pyridin-3-yl}indoline-1-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H19ClN4O2
Molar mass394.86 g·mol−1
3D model (JSmol)
  • Cc1cc2CCN(c2cc1Cl)C(=O)Nc(cc4)cnc4Oc3cccnc3C
  • InChI=1S/C21H19ClN4O2/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27)
  • Key:GIUZEIJUFOPTMR-UHFFFAOYSA-N

SB-242084 is a psychoactive drug and research chemical which acts as a selective antagonist for the 5HT2C receptor. It has anxiolytic effects, and enhances dopamine signalling in the limbic system, as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions but reducing it in others. 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. In animal studies, SB-242084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines.

See also

References

  1. ^ Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, 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. S2CID 23032157.
  2. ^ Martin JR, Ballard TM, Higgins GA (April 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. S2CID 19142495.
  3. ^ Di Matteo V, Di Giovanni G, Di Mascio M, Esposito E (August 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. S2CID 39658512.
  4. ^ Navailles S, De Deurwaerdère P, Porras G, Spampinato U (February 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 (November 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. S2CID 43833462.
  6. ^ Navailles S, Moison D, Cunningham KA, Spampinato U (January 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 (February 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, et al. (October 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 (November 2007). "Acute selective serotonin reuptake inhibitors increase conditioned fear expression: blockade with a 5-HT(2C) receptor antagonist". Biological Psychiatry. 62 (10): 1111–8. doi:10.1016/j.biopsych.2006.11.023. PMC 2129095. PMID 17524369.
  10. ^ Manvich DF, Kimmel HL, Cooper DA, Howell LL (September 2012). "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. doi:10.1124/jpet.112.195156. PMC 3422522. PMID 22685342.
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