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RS-127,445: Wikis

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RS-127,445
Systematic (IUPAC) name
4-(4-fluoro-1-naphthyl)-6-isopropylpyrimidin-2-amine
Identifiers
CAS number 199864-87-4
ATC code  ?
PubChem 196968
Chemical data
Formula C 17H16FN3  
Mol. mass 281.327 g/mol
SMILES eMolecules & PubChem
Synonyms RS-127,445
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

RS-127,445 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x 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-127,445 has been a useful tool in unravelling the function of the various systems in which this receptor is expressed.[2][3][4]

References

  1. ^ 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. PMID 10455251
  2. ^ 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. PMID 12244304
  3. ^ 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
  4. ^ 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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