SB-215,505

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	6603999
ChEMBL	CHEMBL525998
Hemijski podaci
Formula	C19H16ClN3O
Mol. masa	337,803 g/mol
SMILES	eMolekuli & PubHem
InChI
	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
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

SB-215,505 je lek koji deluje kao potentan i selektivan antagonist na serotoninskom 5-HT_2B receptoru, sa dobrom selektivnošću u odnosu na srodne 5-HT_2A i 5-HT_2C receptore.^[4] On se koristi u naučnim istraživanjima funkcije 5-HT₂ familije receptora, a posebno za studiranje uloge 5-HT_2B receptora radu srca,^[5]^[6]^[7] i za razlikovanje 5-HT_2B-posredovanih responsa od onih proizvedenih 5-HT_2A ili 5-HT_2C receptorom.^[8]^[9]^[10]

Reference

↑ 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. edit
↑ 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.
↑ 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
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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. 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

[pmid15265808-4] 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.

[pmid15302781-5] 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.

[pmid16962085-6] 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.

[pmid18591460-7] 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.

[pmid10188965-8] 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.

[pmid12377394-9] 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.

[pmid17673981-10] 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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