SCH 58261

国际站：SCH 58261

CAS：160098-96-4

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：SCH 58261 是一种有效、选择性和竞争性的腺苷 A2A 受体拮抗剂，IC₅₀ 为 15 nM，显示 323-、53-对 A2A 受体的选择性分别比 A1、A2B 和 A3 受体高 100 倍^[1][2][3]。 IC50 和目标：IC50：15 nM（A2A 受体）。

体外：SCH 58261（0 nM–10 µM；7 天）降低 NSCLC 细胞系 H1975 中的浓度依赖性细胞活力^[4]。SCH58261（25 μM；72 小时）可以抑制CAF细胞的生长^[5].

体内：SCH 58261（2 mg/kg；腹腔注射；每天；持续 20 天）在 NSCLC 小鼠模型中引起肿瘤负荷降低^[5]。SCH 58261（5 mg/kg ; ip; 3 次; 每 3 小时; 氟哌啶醇前 10 分钟）部分降低氟哌啶醇诱导的强直性昏厥和纹状体背外侧和腹外侧 PENK mRNA 表达的增加在所有三个检查水平 ^[6] .SCH 58261在大鼠模型中降低帕金森样肌肉僵硬并增强L-DOPA的作用^[7].

参考文献：[1]. Zocchi C, et al. Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes. Br J Pharmacol. 1996 Apr;117(7):1381-6.[2]. Varani K, et al. 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.[3]. Xi J, et al. Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol. 2009 Nov;47(5):684-90.[4]. Kuzumaki N, et al. 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.[5]. Mediavilla-Varela M, et al. Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth. Cancer Biol Ther. 2013 Sep;14(9):860-8.[6]. Wardas J, 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.[7]. Wardas J, et al. SCH 58261, an A(2A) adenosine receptor antagonist, counteracts parkinsonian-like muscle rigidity in rats. Synapse. 2001 Aug;41(2):160-71.