Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetP2X receptor

Target IC₅₀: ~ 1 µM as antagonist of P2X receptor in smooth muscle; 19 nM, 770 nM, 1.62 µM and ﹤300 µM, against P2X1, P2X2, P2X3, P2X4, respectively, in Xenopus oocytes pre-incubated with ATP

Cell permeable: yes

General description

A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC₅₀/K_B ~ 1 µM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no effect on α_1A adrenoceptors, adenosine A₁ and A_2B receptors, histamine H₁, muscarinic M₃ and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X₁ >P2X₂ >P2X₃ >P2X₄ (IC₅₀ = 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 P2X₁ > human P2X₁ > > rat P2X₂ > rat P2X₃ ~ human P2X₇ > > human P2X₄. Not degraded by ecto-nucleotidases.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Klapperstück, M., et al. 2000. Eur. J. Pharmacol.387, 245.Rettinger, J., et al. 2000. Neuropharmacol.39, 2044.Lambrecht, G., et al. 1999. Prog. Brain Res.120,107.Damer, S., et al. 1998. Eur. J. Pharmacol.350, R5.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)