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SB-215505

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SB-215505 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with good selectivity over the related 5-HT2A and 5-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]

SB-215505
Identifiers
  • 6-chloro-5-methyl-N-quinolin-4-yl-2,3-dihydroindole-1-carboxamide
CAS Number
PubChem CID
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)

References

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  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.


 

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