PF-184563

PF-184563
Clinical data
ATC code
  • none
Pharmacokinetic data
Bioavailability34%
Protein binding69%
Elimination half-life1.8h
Identifiers
  • 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
CAS Number
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC21H23ClN6
Molar mass394.91 g·mol−1
3D model (JSmol)
  • CN1CC2=C(C=CC(=C2)Cl)N3C(=NN=C3C4CCN(CC4)C5=CC=CC=N5)C1
  • InChI=1S/C21H23ClN6/c1-26-13-16-12-17(22)5-6-18(16)28-20(14-26)24-25-21(28)15-7-10-27(11-8-15)19-4-2-3-9-23-19/h2-6,9,12,15H,7-8,10-11,13-14H2,1H3 ☒N
  • Key:LXHAZNJVVVBJIF-UHFFFAOYSA-N ☒N
 ☒NcheckY (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

  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, 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". Bioorg. Med. Chem. Lett. 21 (19): 5684–5687. doi:10.1016/j.bmcl.2011.08.038. PMID 21885275.
  2. ^ Brouard R, Bossmar T, Fournie-Lloret D, Chassard D, Akerlund M (2000). "Effect of SR49059, an orally active V1a vasopressin receptor antagonist, in the prevention of dysmenorrhoea". Br. J. Obstet. Gynaecol. 107 (5): 614–619. doi:10.1111/j.1471-0528.2000.tb13302.x. PMID 10826575. S2CID 19439985.
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