Chemical Name:4,4',4'',4'''-[Carbonylbis[imino-5,1,3-benzenetriylbis(
carbonylimino)]]tetrakisbenzenesulfonic acid
tetrasodium salt
Biological Activity:
High affinity P2X3 receptor
antagonist (Ki values are 36, 82 and 4144 nM for P2X3,
P2X1 and P2X2 recombinant receptors respectively). Shows
no activity at P2Y1, P2Y2 and P2Y11 receptors
(IC50 > 10 μM). Potently
inhibits α,β-meATP-evoked
desensitising currents in rat DRG neurons (IC50 = 527 nM). Shows
antitumour activity against several tumour types.
Dharet al (2000) Antitumour
activity of suramin analogues in human tumour cell lines and primary cultures
of tumour cells from patients. Eur.J.Cancer 36 803. Kassacket al (2004) Structure-activity relationships of analogues of NF449
confirm NF449 as the most potent and selective known P2X1 receptor
antagonist. Eur.J.Med.Chem. 39 345. Hausmannet al
(2006) The suramin analog 4,4',4'',4'''-(Carbonylbis(imino-5,1,3-benzenetriylbis
(carbonylimino)))tetra-kis-benzenesulfonic acid (NF110) potently blocks P2X3
receptors: subtype selectivity is determined by location of sulfonic acid
groups. Mol.Pharmacol. 69 2058.