| Bioactivity | GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions[1][2]. | ||||||||||||
| Target | Ki: 3.1 nM (Adenosine A1 receptor) and 1300 nM (Adenosine A2 receptor) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | GR79236 | ||||||||||||
| CAS | 124555-18-6 | ||||||||||||
| Formula | C15H21N5O5 | ||||||||||||
| Molar Mass | 351.36 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. L J Knutsen, et al. N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77. [2]. Sneyd JR, et al. Multicentre evaluation of the adenosine agonist GR79236X in patients with dental pain after third molar extraction. Br J Anaesth. 2007 May;98(5):672-676. [3]. P Strong, et al. Suppression of non-esterified fatty acids and triacylglycerol in experimental animals by the adenosine analogue GR79236. Clin Sci (Lond). 1993 Jun;84(6):663-9. |