PF-184563

Chemical compound
  • none
Pharmacokinetic dataBioavailability34%Protein binding69%Elimination half-life1.8hIdentifiers
  • 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
  • 748806-39-5 checkY
ChemSpider
  • 9412479 ☒N
ChEMBL
  • ChEMBL1837037 ☒N
Chemical and physical dataFormulaC21H23ClN6Molar mass394.91 g·mol−13D model (JSmol)
  • Interactive image
  • CN1CC2=C(C=CC(=C2)Cl)N3C(=NN=C3C4CCN(CC4)C5=CC=CC=N5)C1
InChI
  • 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.
  • v
  • t
  • e
Oxytocin and vasopressin receptor modulators
Oxytocin
Vasopressin
V1A
V1B
  • Ligands: TASP-699
V2
Unsorted
  • Antagonists: Balovaptan
  • Ribuvaptan
  • RWJ-339489
  • VMAX-367
  • VMAX-372
  • VMAX-382
  • YM-222546
Others
Stub icon

This hormonal preparation article is a stub. You can help Wikipedia by expanding it.

  • v
  • t
  • e