SB-215,505

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SB-215,505
(IUPAC) ime
6-hloro-5-metil-N-hinolin-4-il-2,3-dihidroindol-1-karboksamid
Klinički podaci
Identifikatori
CAS broj 162100-15-4
ATC kod nije dodeljen
PubChem[1][2] 6603999
ChEMBL[3] CHEMBL525998 YesY
Hemijski podaci
Formula C19H16ClN3O 
Mol. masa 337,803 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

SB-215,505 je lek koji deluje kao potentan i selektivan antagonist na serotoninskom 5-HT2B receptoru, sa dobrom selektivnošću u odnosu na srodne 5-HT2A i 5-HT2C receptore.[4] On se koristi u naučnim istraživanjima funkcije 5-HT2 familije receptora, a posebno za studiranje uloge 5-HT2B receptora radu srca,[5][6][7] i za razlikovanje 5-HT2B-posredovanih responsa od onih proizvedenih 5-HT2A ili 5-HT2C receptorom.[8][9][10]

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. Kantor S, Jakus R, Balogh B, Benko A, Bagdy G (August 2004). "Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505". British Journal of Pharmacology 142 (8): 1332–42. PMC 1575194. PMID 15265808. doi:10.1038/sj.bjp.0705887. 
  5. Jaffré F, Callebert J, Sarre A, Etienne N, Nebigil CG, Launay JM, Maroteaux L, Monassier L (August 2004). "Involvement of the serotonin 5-HT2B receptor in cardiac hypertrophy linked to sympathetic stimulation: control of interleukin-6, interleukin-1beta, and tumor necrosis factor-alpha cytokine production by ventricular fibroblasts". Circulation 110 (8): 969–74. PMID 15302781. doi:10.1161/01.CIR.0000139856.20505.57. 
  6. Liang YJ, Lai LP, Wang BW, Juang SJ, Chang CM, Leu JG, Shyu KG (November 2006). "Mechanical stress enhances serotonin 2B receptor modulating brain natriuretic peptide through nuclear factor-kappaB in cardiomyocytes". Cardiovascular Research 72 (2): 303–12. PMID 16962085. doi:10.1016/j.cardiores.2006.08.003. 
  7. Monassier L, Laplante MA, Jaffré F, Bousquet P, Maroteaux L, de Champlain J (August 2008). "Serotonin 5-HT(2B) receptor blockade prevents reactive oxygen species-induced cardiac hypertrophy in mice". Hypertension 52 (2): 301–7. PMID 18591460. doi:10.1161/HYPERTENSIONAHA.107.105551. 
  8. Reavill C, Kettle A, Holland V, Riley G, Blackburn TP (February 1999). "Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist". British Journal of Pharmacology 126 (3): 572–4. PMC 1565856. PMID 10188965. doi:10.1038/sj.bjp.0702350. 
  9. Fletcher PJ, Grottick AJ, Higgins GA (October 2002). "Differential effects of the 5-HT(2A) receptor antagonist M100907 and the 5-HT(2C) receptor antagonist SB242084 on cocaine-induced locomotor activity, cocaine self-administration and cocaine-induced reinstatement of responding". Neuropsychopharmacology 27 (4): 576–86. PMID 12377394. doi:10.1016/S0893-133X(02)00342-1. 
  10. Fletcher PJ, Tampakeras M, Sinyard J, Higgins GA (December 2007). "Opposing effects of 5-HT(2A) and 5-HT(2C) receptor antagonists in the rat and mouse on premature responding in the five-choice serial reaction time test". Psychopharmacology 195 (2): 223–34. PMID 17673981. doi:10.1007/s00213-007-0891-z. 

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