Biochem/physiol Actions

Reversible: yes

General description

A cell-permeable adenosine analog that acts a potent non-selective agonist of adenosine receptors (K_i = 14 nM, 20 nM, 2.4 µM and 6.2 nM for A₁, A_2A, A_2B, A₃, respectively). Increases intracellular cAMP production (EC₅₀ = 3.1 µM in A_2B expressing CHO cells). Shown to increase glucagon release in a dose-dependent manner and inhibit insulin release at low concentrations. Although at higher concentration some insulin release is observed. Also, displays a wide range adenosine-dependent effects, such as blocking platelet aggregation and inhibiting DNA synthesis. When administered at reperfusion, it is shown reduce infarction and block the formation of the mitochondrial permeability transition pore by activating p70S6 kinase.

Legal Information

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

Other Notes

Forster, K., et al. 2006. Basic Res. Cardiol.101, 319.de Zwart, M., et al. 1998. Nucleosides Nucleotides.17, 969.Phillis, J. et al. 1986, Pharm. Biochem. Behavior.24, 263 Durcan, M. J., et al. 1989. Pharmacol Biochem Behav.32, 487. Bacher, S., et al. 1982. Naunyn Schmiedebergs Arch Pharmacol.329, 67.Cusack, N., et al. 1981. Br J Pharm.72, 443.Londos, C., et al. 1980. Proc Natl Acad Sci.77, 2551.

Packaging

Packaged under inert gas

10 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)