General Description
A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC
50/K
B ~1 μM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no discernible effects on α
1A adrenoceptors, adenosine A
1 and A
2B receptors, histamine H
1, muscarinic M
3 and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X
1 >P2X
2 >P2X
3 >P2X
4 (IC
50 = 19 nM, 770 nM, 1.62 μM and >300 μM, respectively) in
Xenopus oocytes pre-incubated with ATP. In rat and human tissues, exhibits a potency profile of rat P2X
1 > human P2X
1 ? rat P2X
2 > rat P2X
3 ~human P2X
7 ? human P2X
4. Not degraded by ecto-nucleotidases.
Biological Activity
A potent and selective P2X 1 antagonist (IC 50 = 19 nM). Displays good selectivity over P2X 2 ,(IC 50 = 0.76 μ M), P2X 3 (IC 50 = 1.62 μ M), P2X 4 (IC 50 > 300 μ M), P2Y receptors and ecto-nucleotidases.
