GR79236

GR79236 is a selective agonist of adenosine A₁ receptors (K_is = 3.1 and 1,300 nM for adenosine A₁ and A₂ receptors, respectively, in rat brain).¹ GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC₅₀ = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC₅₀ value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC₅₀ = 0.83 nM).² GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED₅₀s = 0.13 and 0.3 mg/kg, respectively).¹ It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.

WARNING This product is not for human or veterinary use.

1. Knutsen, L.J.S., Lau, J., Petersen, H., et al. N-Substituted adenosines as novel neuroprotective A₁ agonists with diminished hypotensive effects. J. Med. Chem. 42, 3463-3477 (1999).

2. Merkel, L.A., Hawkins, E.D., Colussi, D.J., et al. Cardiovascular and antilipolytic effects of the adenosine agonist GR79236. Pharmacology 51(4), 224-236 (1995).