Biochem/physiol Actions

Reversible: yes

Primary TargetA1

General description

An adenosine analog that acts as a selective, high affinity agonist for Adenosine A1 receptor (A1R) (K_i = 800 pM; 2.3 µM, 18.8 µM, and 42 nM for human A1, A2A, A2B, A3 respectively). Shown to be centrally active following systemic administration and exhibits anti-convulsive effects. Also reported to inhibit adenylate cyclase activity in rat fat cell membrane (IC₅₀ = 33 nM). Diminishes respiratory rhythm, reduces heart rate, and enhances the activity of K_ATP channels. Reduces norepinephrine release by about 50% in untreated and pertussis toxin treated hearts.

Legal Information

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

Other Notes

Burgdorf, C. et al. 2005. J Cardiovasc Pharmacol.45, 1.Klotz, K. N., et al. 2000. Naunyn Schmiedebergs Arch Pharmacol. 362, 382. Mironov, S., et al. 1990. J Neurophysiol.81, 1.Monopoli, A., et al. 1994.Arzneimittelforschung.44, 1305.Concas, A., et al. 1993. J Pharmacol Exp Ther.267, 844.Lohse, M. J., et al. 1988. Nauryn Schmiedebergs Arch Pharmacol.337, 687.Coffin, V. L., et al. 1987. J Pharmacol Exp Ther.241, 76.

Packaging

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)