Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

KF-26777

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
KF-26777
Clinical data
Other namesKF-26777
Identifiers
  • (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC16H18BrN5O
Molar mass376.258 g·mol−1
3D model (JSmol)
  • CCCN(C2=O)C1N=C(c(cc3)ccc3Br)NC1C=4N2CCN=4
  • InChI=1S/C16H16BrN5O/c1-2-8-21-15-12(14-18-7-9-22(14)16(21)23)19-13(20-15)10-3-5-11(17)6-4-10/h3-6H,2,7-9H2,1H3,(H,19,20)
  • Key:GYGNZJDWTHECQT-UHFFFAOYSA-N
  (verify)

KF-26777 is a drug which acts as a potent and selective antagonist for theadenosineA3receptor, with sub-nanomolar affinity (A3Ki=0.2nM) and high selectivity over the other threeadenosine receptor subtypes.[1] Simplexanthine derivatives such ascaffeine andDPCPX have generally low affinity for the A3 subtype and must be extended by expanding the ring system and adding an aromatic group to give high A3 affinity and selectivity.[2]

References

[edit]
  1. ^Saki M, Tsumuki H, Nonaka H, Shimada J, Ichimura M (May 2002). "KF26777 (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride), a new potent and selective adenosine A3 receptor antagonist".European Journal of Pharmacology.444 (3):133–41.doi:10.1016/S0014-2999(02)01662-X.PMID 12063073.
  2. ^Baraldi PG, Tabrizi MA, Gessi S, Borea PA (January 2008). "Adenosine receptor antagonists: translating medicinal chemistry and pharmacology into clinical utility".Chemical Reviews.108 (1):238–63.doi:10.1021/cr0682195.PMID 18181659.
Receptor
(ligands)
P0 (adenine)
P1
(adenosine)
P2
(nucleotide)
P2X
(ATPTooltip Adenosine triphosphate)
P2Y
Transporter
(blockers)
CNTsTooltip Concentrative nucleoside transporters
ENTsTooltip Equilibrative nucleoside transporters
PMATTooltip Plasma membrane monoamine transporter
Enzyme
(inhibitors)
XOTooltip Xanthine oxidase
Others
Others
Retrieved from "https://en.wikipedia.org/w/index.php?title=KF-26777&oldid=1244521916"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp