| CAS NO: | 107756-30-9 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 390.29 |
| Cas No. | 107756-30-9 |
| Formula | C14H19N3O3S·HBr |
| Solubility | Soluble in H2O |
| Chemical Name | (S)-N-(5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)methanesulfonamide hydrobromide |
| Canonical SMILES | OC1=C(C2=C(C=C1)[C@@H](C3=NCCN3)CCC2)NS(=O)(C)=O.Br |
| 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。 |
A 61603 hydrobromide是一种强效的和选择性的α1A肾上腺素受体激动剂[1].
α1A肾上腺素受体(α1A-AR)属于α1肾上腺素能受体,其包括α1A\α1B和α1D三种亚型,并在调节细胞生长和增殖中起重要作用.
A 61603 hydrobromide是一种强效的和选择性的α1A肾上腺素受体激动剂.A-61603对α1A-AR的效力比对α1B-AR或α1D-AR 高35倍.在转染α1A-AR的成纤维细胞中,A-61603显著刺激磷酸肌醇水解[1].A 61603对α1A-AR\α1B-AR和α1D-AR 表现出亲和力,pKi 值分别为8.05/7.52\5.68和5.87.此外,A 61603对α1A-AR\α1B-AR和α1D-AR显示出激动剂活性,pEC50值分别为8.24/7.66\6.50和5.59[2].在新生大鼠心肌细胞中,A61603剂量依赖性地显著增加钙瞬变的频率,EC50值为6.9 nM [3].在分离的小鼠肠系膜血管床中,A61603显著增加灌注压力,比去氧肾上腺素效力强235倍,这表明α1A-AR在血压控制中起重要作用[4].
参考文献：
[1]. Knepper SM, Buckner SA, Brune ME, et al. A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype. J Pharmacol Exp Ther, 1995, 274(1): 97-103.
[2]. Meyer MD, Altenbach RJ, Hancock AA, et al. Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist. J Med Chem, 1996, 39(20): 4116-4119.
[3]. Luo DL, Gao J, Fan LL, et al. Receptor subtype involved in alpha 1-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta Pharmacol Sin, 2007, 28(7): 968-974.
[4]. Martínez-Salas SG1, Campos-Peralta JM, Pares-Hipolito J, et al. Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed. Auton Autacoid Pharmacol, 2007, 27(3): 137-142.
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