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 kôd]

  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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  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. DOI:10.1093/nar/gkr777. PMID 21948594.  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. DOI:10.1038/sj.bjp.0705887. PMC 1575194. PMID 15265808. //www.ncbi.nlm.nih.gov/pmc/articles/PMC1575194/. 
  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. DOI:10.1161/01.CIR.0000139856.20505.57. PMID 15302781. 
  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. DOI:10.1016/j.cardiores.2006.08.003. PMID 16962085. 
  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. DOI:10.1161/HYPERTENSIONAHA.107.105551. PMID 18591460. 
  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. DOI:10.1038/sj.bjp.0702350. PMC 1565856. PMID 10188965. //www.ncbi.nlm.nih.gov/pmc/articles/PMC1565856/. 
  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. DOI:10.1016/S0893-133X(02)00342-1. PMID 12377394. 
  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. DOI:10.1007/s00213-007-0891-z. PMID 17673981. 

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