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Phenoxybenzamine hydrochloride (NCI-c01661) 是一种选择性的 α-adrenoceptor 和 calmodulin 的抑制剂,是常用的抗高血压药。
Phenoxybenzamine hydrochloride (NCI-c01661) 是一种选择性的 α-adrenoceptor 和 calmodulin 的抑制剂,是常用的抗高血压药。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | ¥ 119 | 现货 | |
500 mg | ¥ 249 | 现货 | |
1 g | ¥ 418 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 148 | 现货 |
产品描述 | Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen. |
体外活性 | Phenoxybenzamine hydrochloride对[3H]yohimbine结合的阻断所导出的IC50(100 nM)明显低于其对Noradrenaline 引起的环磷酸腺苷(cyclic AMP)积累效应的逆转IC50(550 nM)[1]。Phenoxybenzamine hydrochloride(50 nM)与Phenoxybenzamine hydrochloridetolamine(1000 nM)联合使用比单独使用Phenoxybenzamine hydrochloride(50 nM)时更能增强Phenoxybenzamine hydrochlorideylephrine诱导的血管收缩,这一效果在完整内皮的主动脉中同样观察到。无论是dexmedetomidine(300或1000 nM)与Phenoxybenzamine hydrochloride(50 nM)的联合使用,还是Phenoxybenzamine hydrochloridetolamine(1000 nM)与Phenoxybenzamine hydrochloride(50 nM)的联合处理,相比单独使用Phenoxybenzamine hydrochloride(50 nM),都能增强Phenoxybenzamine hydrochlorideylephrine引发的收缩反应。此外,与dexmedetomidine(1000 nM)和Phenoxybenzamine hydrochloride的联合使用相比,Phenoxybenzamine hydrochloridetolamine与Phenoxybenzamine hydrochloride的联合使用在增强Phenoxybenzamine hydrochlorideylephrine引起的收缩方面更为显著。高浓度dexmedetomidine(1000 nM)与Phenoxybenzamine hydrochloride的联合使用,比低浓度dexmedetomidine(300 nM)与Phenoxybenzamine hydrochloride的联合使用,更能增强Phenoxybenzamine hydrochlorideylephrine诱发的收缩作用[2]。 |
体内活性 | Phenoxybenzamine hydrochloride(20 nM,皮下注射)有效抑制了小鼠中胶质瘤细胞的肿瘤生成,且Phenoxybenzamine hydrochloride-U87 mg移植瘤的细胞密度显著下降[3]。以Phenoxybenzamine hydrochloride(1 mg/kg,静脉注射)处理的大鼠在神经症状打分(NSS)和足失误评分方面显示出显著改善[4]。 |
细胞实验 | Phenoxybenzamine hydrochloride is dissolved in DMSO. After cytometry, 1×3 cells are implanted in a 96-well plate in 100 μL DMEM supplemented with 10 % FBS. Ten microliter (10 % of the total volume) WST-1 (Water Soluble Tetrazolium) is added to cells and incubated at 37°C for 30 min before colorimetric assay with 450 nm excitation and 630 nm emission at 24 h intervals up to 96 h. The mean fluorescence value is counted, and the cell number is determined using the standard curve. |
别名 | 盐酸酚苄明, 苯氧苯札明, Phenoxybenzamine HCl, NSC 37448, NCI-c01661 |
分子量 | 340.3 |
分子式 | C18H23Cl2NO |
CAS No. | 63-92-3 |
Smiles | Cl.CC(COc1ccccc1)N(CCCl)Cc1ccccc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 63 mg/mL (185.1 mM) H2O: 14 mg/mL (41.1 mM) DMSO: 55 mg/mL (161.62 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
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