Piboserod

Piboserod
(IUPAC) ime
	N-((1-Butil-4-piperidil)-metil)-3,4-dihidro-2H-(1,3)oksazino(3,2-a)indol-10-karboksamid
Klinički podaci
Identifikatori
CAS broj	152811-62-6
ATC kod	nije dodeljen
PubChem	177336
UNII	4UQ3S81B25
ChEMBL	CHEMBL356359
Hemijski podaci
Formula	C22H31N3O2
Mol. masa	369,50 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C22H31N3O2/c1-2-3-11-24-13-9-17(10-14-24)16-23-21(26)20-18-7-4-5-8-19(18)25-12-6-15-27-22(20)25/h4-5,7-8,17H,2-3,6,9-16H2,1H3,(H,23,26) ; Key: KVCSJPATKXABRQ-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Klinička faza II
Način primene	Oralno

Piboserod (Serlipet) je selektivni antagonist 5-HT₄ receptora koji je u prodaji za tretiranje atrijalne fibrilacije i sindroma iritabilnih creva.

Mišići srčanih komora obolelog srca imaju povećanu osetljivost na serotonin.^[4] Do toga dolazi zbog povišenog izražavanja 5-HT₄ receptora u njima. Na osnovu tog nalaza, i po analogiji na efikasnot primene beta blokatora u lečenju zatajenja srca, formirana je hipoteza da 5-HT₄ antagonisti mogu da budu korisni u tretirnaju otkazivanja srca. Ova hipoteza potvrđena na životinjskim modelima.^[5]

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
↑ Bratteli T. et al., Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure. Naunyn-Schmiedeberg's Arch. Pharmacol., 370:157-166, 2004
↑ Birkeland JA. et al., Effects of treatment with a 5-HT4 receptor antagonist in heart failure. Br J Pharmacol. 2007 Jan;150(2):143-52. Epub 2006 Dec 11.

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

[4] Bratteli T. et al., Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure. Naunyn-Schmiedeberg's Arch. Pharmacol., 370:157-166, 2004

[5] Birkeland JA. et al., Effects of treatment with a 5-HT4 receptor antagonist in heart failure. Br J Pharmacol. 2007 Jan;150(2):143-52. Epub 2006 Dec 11.

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