RS-127,445

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RS-127,445
(IUPAC) ime
4-(4-fluoro-1-naftil)-6-izopropilpirimidin-2-amin
Klinički podaci
Identifikatori
CAS broj 199864-87-4
ATC kod nije dodeljen
PubChem[1][2] 196968
Hemijski podaci
Formula C17H16FN3 
Mol. masa 281.327 g/mol
SMILES eMolekuli & PubHem
Sinonimi RS-127,445
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

RS-127,445 je lek koji deluje kao potentan i selektivan antagonist na serotoninskom 5-HT2B receptor, sa oko 1000x selektivnošću u odnosu na blisko srodne 5-HT2A i 5-HT2C receptore.[3] Uloga 5-HT2B receptora u telu još uvek nije dovoljno razjašnjena, i RS-127,445 je bio korisno oruđe u raščlanjavanju funkcija različitih sistema u kojima je ovaj receptor izražen.[4][5][6]

References[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, Chang LK, Pulido-Rios T, Webber A, Leung E, Eglen RM, Martin GR. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. British Journal of Pharmacology. 1999 Jul;127(5):1075-82. DOI:10.1038/sj.bjp.0702632 PMID 10455251
  4. Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L. Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension. Nature Medicine. 2002 Oct;8(10):1129-35. DOI:10.1038/nm764 PMID 12244304
  5. Kelly CR, Sharif NA. Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line. Journal of Pharmacology and Experimental Therapeutics. 2006 Jun;317(3):1254-61. PMID 16517693
  6. Mbaki Y, Ramage AG. Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anaesthetized female rat. British Journal of Pharmacology. 2008 Oct;155(3):343-56. PMID 18604238

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