General description
An adenosine analog that acts as a selective, high affinity agonist for Adenosine A1 receptor (A1R) (Ki = 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 KATP channels. Reduces norepinephrine release by about 50% in untreated and pertussis toxin treated hearts.
Biochem/physiol Actions
Primary Target
A1
Reversible: yes
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51124104
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 119136-10MG
