Biochem/physiol Actions

Reversible: yes

Primary TargetA2A

General description

A highly potent, selective, non-xanthine adenosine A2A receptor antagonist (K_i = 800 pM for human adenosine A2AR stably expressed in HEK-293 cells).

A highly potent, selective, and orally bioavailable non-xanthine adenosine A_2A receptor antagonist (K_i = 800 pM for human adenosine A_2AR stably expressed in HEK-293 cells). Does not exhibit any significant antagonistic activity in A₁, A_2B (K_i = 255 nM and 50 nM, respectively in human adenosine receptors stably expressed in CHO cells) or in A₃R (K_i >10 µM in human A₃R stably expressed in HEK-293 cells). Shown to have a protective effect against beta-amyloid peptide toxicity.

Legal Information

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

Other Notes

Poucher, S. M., et al. 1995. Brit. J. Pharmacol. 115, 1096.Ongini, E. et al. 1999. Naunyn Schmiedebergs Arch Pharmacol. 359, 7.r>Keddie, J. et al. 1996, Eur Journ Pharm. 301, 107.

Packaging

5 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)