GR79236

• CAT Number: I000974
• CAS Number: 124555-18-6
• Molecular Formula: C15H21N5O5
• Molecular Weight: 351.36
• Purity: ≥95%
• Target: Adenosine Receptor
• Solubility: 100 mM in H2O
• Storage: Desiccate at +4C
• IC50: 3.1 nM(Ki)
• InChI: InChI=1S/C15H21N5O5/c21-4-9-11(23)12(24)15(25-9)20-6-18-10-13(16-5-17-14(10)20)19-7-2-1-3-8(7)22/h5-9,11-12,15,21-24H,1-4H2,(H,16,17,19)/t7-,8-,9+,11+,12+,15+/m0/s1
• InChIKey: GYWXTRVEUURNEW-TVDBPQCTSA-N
• SMILES: O[C@H]1[C@H](N2C=NC3=C(N[C@@H]4[C@@H](O)CCC4)N=CN=C23)O[C@H](CO)[C@H]1O

GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.IC50 value: 3.1 nM(Ki)Target: adenosine A1 receptorin vitro: GR79236 is a highly potent and selective A1-receptor agonist that is originally developed for the treatment of Type 2 diabetes mellitus, as a cardioprotective agent and also for peripheral arterial occlusive diseases.in vivo: GR79236 has also been shown to have antinociceptive and anti-inflammatory properties in animal models. GR79236 inhibits the release of CGRP evoked by superior sagittal sinus (SSS) stimulation in the cat and inhibits trigeminal nucleus firing in the cat and rat. GR79236X has acute, short-term analgesic efficacy.

Reference

1:Lack of effect of the adenosine A1 receptor agonist, GR79236, on capsaicin-induced CGRP release in anaesthetized pigs. Arulmani U, Heiligers JP, Centurión D, Garrelds IM, Villalón CM, Saxena PR.Cephalalgia. 2005 Nov;25(11):1082-90. PMID: 16232161 2:Effect of the adenosine A1 receptor agonist GR79236 on trigeminal nociception with blink reflex recordings in healthy human subjects. Giffin NJ, Kowacs F, Libri V, Williams P, Goadsby PJ, Kaube H.Cephalalgia. 2003 May;23(4):287-92. PMID: 12716347 3:The effect of body temperature on myocardial protection conferred by ischaemic preconditioning or the selective adenosine A1 receptor agonist GR79236, in an anaesthetized rabbit model of myocardial ischaemia and reperfusion. Sheldrick A, Gray KM, Drew GM, Louttit JB.Br J Pharmacol. 1999 Sep;128(2):385-95. PMID: 10510449 Free PMC Article4:The time course of cardioprotection induced by GR79236, a selective adenosine A1-receptor agonist, in myocardial ischaemia-reperfusion injury in the pig. Louttit JB, Hunt AA, Maxwell MP, Drew GM.J Cardiovasc Pharmacol. 1999 Feb;33(2):285-91. PMID: 10028938 5:Adenosine A1 receptor agonist GR79236 suppresses apnea during all sleep stages in the rat. Carley DW, Hagan RM, Sheehan M, Trbovic S, Thai T, Radulovacki M.Sleep. 1997 Dec;20(12):1093-8. PMID: 9493917 6:Short-term metabolic and haemodynamic effects of GR79236 in normal and fructose-fed rats. Qu X, Cooney G, Donnelly R.Eur J Pharmacol. 1997 Nov 12;338(3):269-76. PMID: 9424021 7:In vitro effect of adenosine agonist GR79236 on the insulin sensitivity of glucose utilisation in rat soleus and human rectus abdominus muscle. Webster JM, Heseltine L, Taylor R.Biochim Biophys Acta. 1996 Jun 7;1316(2):109-13. PMID: 8672547 Free Article8:Cardiovascular and antilipolytic effects of the adenosine agonist GR79236. Merkel LA, Hawkins ED, Colussi DJ, Greenland BD, Smits GJ, Perrone MH, Cox BF.Pharmacology. 1995 Oct;51(4):224-36. PMID: 8577816 9:The effects of GR79236 on plasma fatty acid concentrations, heart rate and blood pressure in the conscious rat. Gardner CJ, Twissell DJ, Coates J, Strong P.Eur J Pharmacol. 1994 May 12;257(1-2):117-21. PMID: 8082691 10:Suppression of non-esterified fatty acids and triacylglycerol in experimental animals by the adenosine analogue GR79236. Strong P, Anderson R, Coates J, Ellis F, Evans B, Gurden MF, Johnstone J, Kennedy I, Martin DP.Clin Sci (Lond). 1993 Jun;84(6):663-9. PMID: 8334813