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.[1] On se koristi u naučnim istraživanjima funkcije 5-HT2 familije receptora, a posebno za studiranje uloge 5-HT2B receptora radu srca,[2][3][4] i za razlikovanje 5-HT2B-posredovanih responsa od onih proizvedenih 5-HT2A ili 5-HT2C receptorom.[5][6][7]

SB-215,505
IUPAC ime
6-hloro-5-metil-N-hinolin-4-il-2,3-dihidroindol-1-karboksamid
Identifikatori
CAS broj162100-15-4 ДаY
ATC kodnone
PubChemCID 6603999
ChEMBLCHEMBL525998 ДаY
Hemijski podaci
FormulaC19H16ClN3O
Molarna masa337,803 g/mol
  • CC1=C(C=C2C(=C1)CCN2C(=O)NC3=CC=NC4=CC=CC=C43)Cl

Reference

уреди
  1. ^ Kantor S, Jakus R, Balogh B, Benko A, Bagdy G (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. 
  2. ^ Jaffré F, Callebert J, Sarre A, Etienne N, Nebigil CG, Launay JM, Maroteaux L, Monassier L (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. 
  3. ^ Liang YJ, Lai LP, Wang BW, Juang SJ, Chang CM, Leu JG, Shyu KG (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. 
  4. ^ Monassier L, Laplante MA, Jaffré F, Bousquet P, Maroteaux L, de Champlain J (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. 
  5. ^ Reavill C, Kettle A, Holland V, Riley G, Blackburn TP (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. 
  6. ^ Fletcher PJ, Grottick AJ, Higgins GA (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. 
  7. ^ Fletcher PJ, Tampakeras M, Sinyard J, Higgins GA (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. 

Spoljašnje veze

уреди