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RS-127445





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(Redirected from RS-127,445)
  

RS-127445 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000 times selectivity over the closely related 5-HT2A and 5-HT2C receptors.[1] The role of the 5-HT2B receptor in the body is still poorly understood, and RS-127445 has been a useful tool in unravelling the function of the various systems in which this receptor is expressed.[2][3][4]

RS-127445
Clinical data
Other namesRS-127,445
Identifiers

  • 4-(4-fluoro-1-naphthyl)-6-isopropylpyrimidin-2-amine

CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H16FN3
Molar mass281.334 g·mol−1
3D model (JSmol)

  • Nc3nc(C(C)C)cc(n3)-c(cc2)c1ccccc1c2F

  • InChI=1S/C17H16FN3/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13/h3-10H,1-2H3,(H2,19,20,21)

  • Key:ZZZQXCUPAJFVBN-UHFFFAOYSA-N

  (verify)

References

edit
  1. ^ Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, et al. (July 1999). "RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist". British Journal of Pharmacology. 127 (5): 1075–82. doi:10.1038/sj.bjp.0702632. PMC 1566110. PMID 10455251.
  • ^ Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, et al. (October 2002). "Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension" (PDF). Nature Medicine. 8 (10): 1129–35. doi:10.1038/nm764. PMID 12244304. S2CID 20736218.
  • ^ Kelly CR, Sharif NA (June 2006). "Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line". The Journal of Pharmacology and Experimental Therapeutics. 317 (3): 1254–61. doi:10.1124/jpet.105.100172. PMID 16517693. S2CID 6604193.
  • ^ Mbaki Y, Ramage AG (October 2008). "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. 155 (3): 343–56. doi:10.1038/bjp.2008.273. PMC 2567885. PMID 18604238.
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    Last edited on 10 May 2024, at 13:35  





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