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SB-215505

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
SB-215505
Identifiers
  • 6-chloro-5-methyl-N-quinolin-4-yl-2,3-dihydroindole-1-carboxamide
CAS Number
PubChemCID
ChemSpider
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC19H16ClN3O
Molar mass337.81 g·mol−1
3D model (JSmol)
  • CC1=C(C=C2C(=C1)CCN2C(=O)NC3=CC=NC4=CC=CC=C43)Cl
  • InChI=1S/C19H16ClN3O/c1-12-10-13-7-9-23(18(13)11-15(12)20)19(24)22-17-6-8-21-16-5-3-2-4-14(16)17/h2-6,8,10-11H,7,9H2,1H3,(H,21,22,24)
  • Key:BPVGSWDWIRIUME-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

SB-215505 is a drug which acts as a potent and selectiveantagonist at theserotonin5-HT2Breceptor, with good selectivity over the related5-HT2A and5-HT2C receptors.[1] It is used in scientific research into the function of the 5-HT2 family of receptors, especially to study the role of 5-HT2B receptors in the heart,[2][3][4] and to distinguish 5-HT2B-mediated responses from those produced by 5-HT2A or 5-HT2C.[5][6][7]

References

[edit]
  1. ^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.
  2. ^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"(PDF).Circulation.110 (8):969–74.doi:10.1161/01.CIR.0000139856.20505.57.PMID 15302781.
  3. ^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.
  4. ^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.
  5. ^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.
  6. ^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.
  7. ^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.S2CID 8334076.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7


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