Chemistry:RS-127445

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Short description: Chemical compound
RS-127445
RS-127,445 structure.png
Clinical data
Other namesRS-127,445
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC17H16FN3
Molar mass281.334 g·mol−1
3D model (JSmol)
  (verify)

RS-127445 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-127445 has been a useful tool in unravelling the function of the various systems in which this receptor is expressed.[2][3][4]

References

  1. ↑ "RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist". British Journal of Pharmacology 127 (5): 1075–82. July 1999. doi:10.1038/sj.bjp.0702632. PMID 10455251. 
  2. ↑ "Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension". Nature Medicine 8 (10): 1129–35. October 2002. doi:10.1038/nm764. PMID 12244304. https://hal.archives-ouvertes.fr/hal-01985063/file/NM_final_rev.pdf. 
  3. ↑ "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. June 2006. doi:10.1124/jpet.105.100172. PMID 16517693. 
  4. ↑ "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. October 2008. doi:10.1038/bjp.2008.273. PMID 18604238. 



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