Chemical Name:8,8'-[carbonylbis(imino-3,1-phenylenecarbonylimino)]bis
-1,3,5-naphthalene-trisulphonic acid, hexasodium salt
Biological Activity:
A
subtype selective, competitive and reversible P2X1 receptor antagonist. Displays IC50 values of
0.21, 28.9, > 50 and > 100 μM for human P2X1, P2X3,
P2X2, and P2X4-mediated responses respectively. Selective
over adrenoceptors, histamine and P2Y receptors. Also selectively inhibits the α-subunit of Go/i (EC50~300 nM).
Van Rheeet al (1994) Novel competitive antagonists for P2
purinoceptors. Eur.J.Pharmacol.Mol.Pharmacol.Sect. 268 1. Freissmuthet al (1996) Suramin analogues as subtype-selective G protein
inhibitors. Mol.Pharmacol. 49 602. Sotoet al
(1999) Antagonistic properties of the suramin analogue NF023 at heterologously
expressed P2X receptors. Neuropharmacology 38 141. Sneddonet al (2000) The effect of P2 receptor antagonists and ATPase
inhibition on sympathetic purinergic neurotransmission in the guinea-pig
isolated vas deferens. Br.J.Pharmacol. 129 1089.
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