Merck, 119149-5MG, Adenosine A2A Receptor Antagonist I, ZM 241385

General description
A highly potent, selective, and orally bioavailable non-xanthine adenosine A₂A receptor antagonist (Ki = 800 pM for human adenosine A₂AR stably expressed in HEK-293 cells). Does not exhibit any significant antagonistic activity in A₁, A₂B (Ki = 255 nM and 50 nM, respectively in human adenosine receptors stably expressed in CHO cells) or in A₃R (Ki >10 µM in human A₃R stably expressed in HEK-293 cells). Shown to have a protective effect against beta-amyloid peptide toxicity.
A highly potent, selective, non-xanthine adenosine A2A receptor antagonist (Ki = 800 pM for human adenosine A2AR stably expressed in HEK-293 cells).
Biochem/physiol Actions
Primary Target
A2A
Reversible: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Poucher, S. M., et al. 1995. Brit. J. Pharmacol. 115, 1096.
Ongini, E. et al. 1999. Naunyn Schmiedebergs Arch Pharmacol. 359, 7.
Keddie, J. et al. 1996, Eur Journ Pharm. 301, 107.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)