| CAS NO: | 55974-42-0 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | White solid |
| Storage | Store at RT |
| M.Wt | 480.43 |
| Cas No. | 55974-42-0 |
| Formula | C24H29N3O3·2HCl |
| Solubility | <48.04mg/ml in H2O |
| Chemical Name | 2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-4,4-dimethylisoquinoline-1,3(2H,4H)-dione dihydrochloride |
| Canonical SMILES | CC(C1=CC=CC=C1C(N2CCN3CCN(C4=CC=CC=C4OC)CC3)=O)(C2=O)C.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
ARC 239 dihydrochloride是一种选择性的α2B肾上腺素受体拮抗剂,pKD值为8.8 [1].
α2B肾上腺素受体是一种G蛋白偶联受体.α2肾上腺素能受体包括α2A\α2B和α2C三种亚型,在调节中枢神经系统肾上腺素能神经元和交感神经释放神经递质中起重要作用.
ARC 239 dihydrochloride是一种选择性的α2B肾上腺素受体拮抗剂.在大鼠脑中,ARC 239抑制5-HTIA受体的放射性配体8-OH-DPAT和RX 821002与皮质膜的结合,Ki值分别为63.1和136 nM,这表明ARC 239识别5-HT1A受体[2].用ARC 239处理人血小板,显著抑制二磷酸腺苷(ADP)\肾上腺素和花生四烯酸诱导的血小板聚集,并增加胶原/肾上腺素闭合时间,这表明α2B肾上腺素受体在血小板聚集中起关键作用[3].在分离自怀孕大鼠的宫颈样本中,ARC 239有效抑制去甲肾上腺素刺激的收缩[4].
在酸化乙醇诱发胃粘膜损伤的C57BL/6小鼠中,ARC 239(10.4 nM)拮抗α2肾上腺素受体激动剂诱导的胃保护作用[5].
参考文献：
[1]. Bylund DB, Ray-Prenger C, Murphy TJ. Alpha-2A and alpha-2B adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype. J Pharmacol Exp Ther, 1988, 245(2): 600-607.
[2]. Meana JJ, Callado LF, Pazos A, et al. The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. Eur J Pharmacol, 1996, 312(3): 385-388.
[3]. Marketou ME, Kintsurashvili E, Androulakis NE, et al. Blockade of platelet alpha2B-adrenergic receptors: a novel antiaggregant mechanism. Int J Cardiol, 2013, 168(3): 2561-2566.
[4]. Gál A, Kolarovszki-Sipiczki Z, et al. The effect of the ARC 239 on the myometrial and cervical action in the rat, in vitro. Acta Pharm Hung, 2009, 79(2): 75-80.
[5]. Zádori ZS, Shujaa N, Brancati SB, et al. Both α2B- and α2C-adrenoceptor subtypes are involved in the mediation of centrally induced gastroprotection in mice. Eur J Pharmacol, 2011, 669(1-3): 115-120.
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