GR79236

GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a K_is of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions^[1][2]. IC50 & Target: Ki: 3.1 nM (Adenosine A1 receptor) and 1300 nM (Adenosine A2 receptor)^[1] In Vitro: GR79236 inhibits Isoprenaline-stimulated cAMP accumulation in DDT-MF2 cells with an IC₅₀ of 2.6 nM^[1].
GR79236 inhibits catecholamine-induced lipolysis in human, rat and dog isolated adipocytes^[3]. In Vivo: GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED₅₀s of 0.13 mg/kg and 0.3 mg/kg, respectively)^[1].
Oral administration of GR79236 (0.1-10 mg/kg) to fed rats induces minimal changes in the plasma concentration of non-esterified fatty acids and in the blood concentrations of glucose and lactate^[3].
Intravenous infusion of GR79236 to fasted pithed rats, or oral administration of GR79236 to fasted conscious rats and dogs, produces time- and dose-dependent decreases in the plasma non-esterified fatty acid concentration. In the fasted rats, doses of GR79236 that lowered plasma levels of non-esterified fatty acids also produced hypotriglyceridaemia and anti-ketotic effects^[3].