SCH 58261

• CAT Number: I002036
• CAS Number: 160098-96-4
• Molecular Formula: C18H15N7O
• Molecular Weight: 345.4
• Purity: ≥95%
• Synonyms: 2-(furan-2-yl)-7-phenethyl-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
• Target: Adenosine Receptor
• Solubility: Soluble to 100 mM in DMSO
• Storage: Store at RT
• InChIKey: UTLPKQYUXOEJIL-UHFFFAOYSA-N

SCH 58261 is the adenosine A2A receptor competitive antagonist. Displays 323-, 53- and 100-fold selectivity over A1, A2B and A3 receptors, respectively.target: adenosine A2A receptorIC50: 15 nM [3]in vitro: NK cells were cultured in NK cell media and preincubated with or without 1 uM SCH58261 30 min before simulation with indicated concentrations of IL-18 (R & D Systems) and IL-12p70 (Australian Biosearch) in the presence or absence of NECA (1 uM) or CGS-21680 (100 nM).[1]in vivo: it was demonstrated that the selective antagonist of the A2Areceptor, SCH58261, administered i.p. starting from the early minutes after ischemia induction, reduces ischemic brain damage and neurological deficit 24 h thereafter. vehicle-rats received saline with Tween 80 (1 %) administered (i.p.) .SCH58261 (0.01 mg/kg, i.p.), administered twice/day for 7 days [2]

Reference

1:Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists. Shah U, Boyle CD, Chackalamannil S, Neustadt BR, Lindo N, Greenlee WJ, Foster C, Arik L, Zhai Y, Ng K, Wang S, Monopoli A, Lachowicz JE.Bioorg Med Chem Lett. 2008 Jul 15;18(14):4199-203. doi: 10.1016/j.bmcl.2008.05.074. Epub 2008 May 22. PMID: 18562199 2:Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists. Shah U, Lankin CM, Boyle CD, Chackalamannil S, Greenlee WJ, Neustadt BR, Cohen-Williams ME, Higgins GA, Ng K, Varty GB, Zhang H, Lachowicz JE.Bioorg Med Chem Lett. 2008 Jul 15;18(14):4204-9. doi: 10.1016/j.bmcl.2008.05.069. Epub 2008 May 22. PMID: 18558486 3:Behavioral and electrophysiological effects of the adenosine A2A receptor antagonist SCH 58261 in R6/2 Huntington/’s disease mice. Domenici MR, Scattoni ML, Martire A, Lastoria G, Potenza RL, Borioni A, Venerosi A, Calamandrei G, Popoli P.Neurobiol Dis. 2007 Nov;28(2):197-205. Epub 2007 Jul 24. PMID: 17720507 4:The selective A2A receptor antagonist SCH 58261 protects from neurological deficit, brain damage and activation of p38 MAPK in rat focal cerebral ischemia. Melani A, Gianfriddo M, Vannucchi MG, Cipriani S, Baraldi PG, Giovannini MG, Pedata F.Brain Res. 2006 Feb 16;1073-1074:470-80. Epub 2006 Jan 26. PMID: 16443200 5:Synergistic effect of SCH 58261, an adenosine A2A receptor antagonist, and L-DOPA on the reserpine-induced muscle rigidity in rats. Wardas J.Pol J Pharmacol. 2003 Mar-Apr;55(2):155-64. PMID: 12926542 Free Article6:SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum. Wardas J, Pietraszek M, Dziedzicka-Wasylewska M.Brain Res. 2003 Jul 11;977(2):270-7. PMID: 12834887 7:The selective A2A receptor antagonist SCH 58261 reduces striatal transmitter outflow, turning behavior and ischemic brain damage induced by permanent focal ischemia in the rat. Melani A, Pantoni L, Bordoni F, Gianfriddo M, Bianchi L, Vannucchi MG, Bertorelli R, Monopoli A, Pedata F.Brain Res. 2003 Jan 10;959(2):243-50. PMID: 12493612 8:SCH 58261 differentially influences quinolinic acid-induced effects in striatal and in hippocampal slices. Tebano MT, Domenici MR, Popoli P.Eur J Pharmacol. 2002 Aug 30;450(3):253-7. PMID: 12208317 9:In vivo labelling of the adenosine A2A receptor in mouse brain using the selective antagonist [3H]SCH 58261. El Yacoubi M, Ledent C, Parmentier M, Ongini E, Costentin J, Vaugeois JM.Eur J Neurosci. 2001 Nov;14(9):1567-70. PMID: 11722618 10:SCH 58261 (an adenosine A(2A) receptor antagonist) reduces, only at low doses, K(+)-evoked glutamate release in the striatum. Pintor A, Quarta D, Pèzzola A, Reggio R, Popoli P.Eur J Pharmacol. 2001 Jun 15;421(3):177-80. PMID: 11516434