PF-184563

PF-184563
Clinical data

ATC code	none
Pharmacokinetic data
Bioavailability	34%
Protein binding	69%
Biological half-life	1.8h
Identifiers
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
CAS Number	748806-39-5^Y
ChemSpider	9412479^N
ChEMBL	CHEMBL1837037^N
Chemical and physical data
Formula	C₂₁H₂₃ClN₆
Molar mass	394.91
3D model (Jmol)	Interactive image
SMILES 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
^NY (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

↑ 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". Bioorganic. Med. Chem. Lett. (21): 5684–5687. doi:10.1016/j.bmcl.2011.08.038. PMID 21885275.
↑ 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. 5 (107): 614–619. doi:10.1111/j.1471-0528.2000.tb13302.x. PMID 10826575.

Oxytocin and vasopressin receptor modulators

Oxytocin

Agonists: Peptide: Aspartocin
Carbetocin
Cargutocin
Demoxytocin
Lipo-oxytocin-1
Merotocin
Nacartocin
Oxytocin
PF-06478939
PF-06655075 (PF1)
TGOT
Vasotocin (argiprestocin); Non-peptide: TC OT 39
WAY-267464

Antagonists: Peptide: Atosiban
Tocinoic acid; Non-peptide: Barusiban
Epelsiban
Erlosiban
IX-01
L-368,899
L-371,257
L-372,662
Retosiban
SSR-126768
WAY-162720

Vasopressin

V_1A	Agonists: Felypressin Lypressin Ornipressin Selepressin Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LY-307174 PF-184563 Relcovaptan RG7314 SRX246 SRX251 TC OT 39 WAY-267464 YM-218 YM-471 YM-35471

V_1B	Agonists: Desmopressin Felypressin Lypressin Ornipressin Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: ABT-436 Nelivaptan ORG-52186

V₂	Agonists: Desmopressin Felypressin Lypressin Ornipressin TC OT 39 Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: Conivaptan JNJ-17079166 Lixivaptan Mozavaptan RWJ-351647 Satavaptan Tolvaptan YM-471 YM-35471

Unsorted	Antagonists: Ribuvaptan RWJ-339489 VMAX-367 VMAX-372 VMAX-382 YM-222546 Other inhibitors: Demeclocycline Lithium (lithium carbonate)

Others

Carrier proteins: Neurophysin (I, II)

See also: Peptide receptor modulators

This article is issued from Wikipedia - version of the 6/4/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.