PF-184563

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PF-184563
PF-184563.png
Systematic (IUPAC) name
8-Chloro-5-methyl-1-(3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4-yl)-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene
Clinical data
Legal status
?
Pharmacokinetic data
Bioavailability 34%
Protein binding 69%
Half-life 1.8h
Identifiers
CAS number 748806-39-5 YesY
ATC code None
ChemSpider 9412479 N
ChEMBL CHEMBL1837037 N
Chemical data
Formula C21H23ClN6 
Molecular mass 394.91
 N (what is this?)  (verify)

PF-184563 is a potent, selective non-peptidic antagonist of the V1a receptor.[1] The compound was discovered by Pfizer in its Sandwich, Kent research center, as a potential treatment for dysmenorrhoea, an indication for which V1a antagonists have shown efficacy.[2]

References[edit]

  1. ^ Johnson PS, Ryckmans T, Bryans J, Beal DM, Dack KN, Feeder N, Harrison A, Lewis M, Mason HJ, Mills J, Newman J, Pasquinet C, Rawson DJ, Roberts LR, Russell R, Spark D, Stobie A, Underwood TJ, Ward R and Wheeler S (October 2011). "Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability". Bioorganic. Med. Chem. Lett. (21): 5684–5687. doi:10.1016/j.bmcl.2011.08.038. PMID 21885275. 
  2. ^ Brouard R, Bossmar T, Fournie-Lloret D, Chassard D and Akerlund M (2000). "Effect of SR49059, an orally active V1a vasopressin receptor antagonist, in the prevention of dysmenorrhoea". Br. J. Obstet. Gynaecol. 5 (107): 614–619. doi:10.1111/j.1471-0528.2000.tb13302.x. PMID 10826575.