SB-242,084

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SB-242,084
(IUPAC) ime
6-hloro-5-metil-N-{6-[(2-metilpiridin-3-il)oksi]piridin-3-il]indolin-1-karboksamid
Klinički podaci
Identifikatori
CAS broj 181632-25-7
ATC kod nije dodeljen
PubChem[1][2] 3644637
ChEMBL[3] CHEMBL14563
Hemijski podaci
Formula C21H19ClN4O2 
Mol. masa 394,853 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

SB-242,084 je psihoaktivni lek i istraživačka hemikalija koja deluje kao selektivni antagonist za 5HT2C receptor.[4] On ima anksiolitičko dejstvo,[5] i pojačava dopaminsku signalizaciju u limbičnom sistemu.[6] On takođe ima kompleksno dejstvo na otpuštanje dopamina proizvedeno kokainom, povećavajući ga u pojedinim delovima mozga[7][8] i snižavajući ga u drugim.[9][10] Pokazano je da povišava efektivnost selektivnih inhibitora preuzimanja serotonina (SSRI), i da redukuje njihove nuspojave.[11][12] U životinjskim studijama, SB-242,084 proizvodi stimulansnu aktivnost, koja je donekle slična ali znatno slabija od kokaina i amfetamina.[13]

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Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  4. Kennett, GA; Wood, MD; Bright, F; Trail, B; Riley, G; Holland, V; Avenell, KY; Stean, T; Upton, N (1997). "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist". Neuropharmacology 36 (4–5): 609–20. PMID 9225286. doi:10.1016/S0028-3908(97)00038-5. 
  5. 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. PMID 11888553. doi:10.1016/S0091-3057(01)00713-4. 
  6. 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. PMID 10462132. doi:10.1016/S0028-3908(99)00047-7. 
  7. 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. PMID 14560323. doi:10.1038/sj.npp.1300329. 
  8. 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. PMID 17018023. doi:10.1111/j.1471-4159.2006.04188.x. 
  9. 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. PMID 17429406. doi:10.1038/sj.npp.1301414. 
  10. 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. PMC 3130963. PMID 18977370. doi:10.1016/j.neuropharm.2008.10.005. 
  11. Cremers, TI; Giorgetti, M; Bosker, FJ; Hogg, S; Arnt, J; Mørk, A; Honig, G; Bøgesø, KP; Westerink, BH (2004). "Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade". Neuropsychopharmacology 29 (10): 1782–9. PMID 15138437. doi:10.1038/sj.npp.1300474. 
  12. 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. PMC 2129095. PMID 17524369. doi:10.1016/j.biopsych.2006.11.023. 
  13. 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. PMID 22685342. doi:10.1124/jpet.112.195156. 

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