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SCH58261

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Chemical Structure| 160098-96-4 同义名 : -
CAS号 : 160098-96-4
货号 : A144938
分子式 : C18H15N7O
纯度 : 99%+
分子量 : 345.358
MDL号 : MFCD00933778
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(101.34 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

4% DMSO40% PEG 300+4% Tween 80++water 2 mg/mL

生物活性
靶点

  • Adenosine Receptor

    bovine A2a, Ki:2.0 nM

    rat A2a, Ki:2.3 nM
描述 Adenosine modulates a variety of physiological functions acting via specific cell surface receptors which are divided into at least four subtypes: A1, A2a, A2b and A3. The A2a receptor subtype which is coupled to stimulation of adenylyl cyclase, is a high affinity receptor found in large amounts in the brain striatum. In the periphery, the A2a receptor is localized in different organs and tissues, including platelets, neutrophils and vascular smooth muscle cells [10]. SCH 58261 is an efficient and selective A2a adenosine receptor antagonist, with Ki values of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively, and displays 50- to 100-fold more selective for A2a receptor than A1, and shows no affinity for either the A3 adenosine receptor or other receptors at concentrations up to 1 mM in rat and bovine brain, respectively [11]. SCH 58261 (0 nM–10 µM; 7 days) decreases cell viability in a concentration-dependent in the NSCLC cell line H1975 [12]. It also antagonized competitively the effects induced by the A2a adenosine-selective agonist CGS 21680 in two functional assays, such as inhibition of rabbit platelet aggregation and porcine coronary artery relaxation [13]. SCH58261, systemically administered (0.01 mg/kg intraperitoneal. 1, 6 and 10 hours after spinal cord injury (SCI)), reduced demyelination and levels of TNF-α, Fas-L, PAR, Bax expression and activation of JNK mitogen-activated protein kinase (MAPK) 24 hours after SCI [14]. 6-OHDA (8 μg/rat, Intra-SNc) induced motor disorders of Parkinson's disease and increased elapsed time in the beam test (p<0.001). Injection of SCH-58261 (2 mg/kg, i.p.) attenuated elapsed time on beam (p<0.01 and p<0.001), which indicated administration of SCH-58261 can improve the 6-OHDA-induced bradykinesia and motor disturbance [15].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.48mL

2.90mL

1.45mL

28.96mL

5.79mL

2.90mL
参考文献

[1]Paterniti I, Melani A, et al. Selective adenosine A2A receptor agonists and antagonists protect against spinal cord injury through peripheral and central effects. J Neuroinflammation. 2011 Apr 12;8:31.

[2]Zocchi C, Ongini E, et al. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.

[3]Pagnussat N, Almeida AS, et al. Adenosine A(2A) receptors are necessary and sufficient to trigger memory impairment in adult mice. Br J Pharmacol. 2015 Aug;172(15):3831-45.

[4]Hsu CW, Wang CS, et al. Caffeine and a selective adenosine A2A receptor antagonist induce sensitization and cross-sensitization behavior associated with increased striatal dopamine in mice. J Biomed Sci. 2010 Jan 15;17:4.

[5]El Yacoubi M, Ledent C, et al. SCH 58261 and ZM 241385 differentially prevent the motor effects of CGS 21680 in mice: evidence for a functional 'atypical' adenosine A(2A) receptor. Eur J Pharmacol. 2000 Jul 28;401(1):63-77.

[6]Popoli P, Pintor A, et al. Blockade of striatal adenosine A2A receptor reduces, through a presynaptic mechanism, quinolinic acid-induced excitotoxicity: possible relevance to neuroprotective interventions in neurodegenerative diseases of the striatum. J Neurosci. 2002 Mar 1;22(5):1967-75.

[7]Wardas J, Pietraszek M, et al. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum. Brain Res. 2003 Jul 11;977(2):270-7.

[8]Leite MR, Wilhelm EA, et al. Protective effect of caffeine and a selective A2A receptor antagonist on impairment of memory and oxidative stress of aged rats. Exp Gerontol. 2011 Apr;46(4):309-15.

[9]Yang M, Soohoo D, et al. Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonists. Naunyn Schmiedebergs Arch Pharmacol. 2007 Apr;375(2):133-44. Epub 2007 Feb 20.

[10]Varani K. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol. 1996 Apr;117(8):1693-701.

[11]Zocchi C. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.

[12]Kuzumaki N. Multiple analyses of G-protein coupled receptor (GPCR) expression in the development of gefitinib-resistance in transforming non-small-cell lung cancer. PLoS One. 2012;7(10):e44368. doi: 10.1371/journal.pone.0044368.

[13] Zocchi C. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.

[14]Paterniti I. Selective adenosine A2A receptor agonists and antagonists protect against spinal cord injury through peripheral and central effects. J Neuroinflammation. 2011 Apr 12;8:31. doi: 10.1186/1742-2094-8-31.

[15]Reyhani-Rad S, Mahmoudi J. Effect of adenosine A2A receptor antagonists on motor disorders induced by 6-hydroxydopamine in rat. Acta Cir Bras. 2016 Feb;31(2):133-7.