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Phenoxybenzamine HCl

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Chemical Structure| 63-92-3 同义名 : Phenoxybenzamine (hydrochloride);NSC 37448;NCI-c01661;Phenoxybenzamine hydrochloride
CAS号 : 63-92-3
货号 : A398762
分子式 : C18H23Cl2NO
纯度 : 98%
分子量 : 340.287
MDL号 : MFCD00055152
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(308.56 mM)，配合低频超声助溶，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：
生物活性
靶点

  • α-adrenergic receptor
描述 Phenoxybenzamine hydrochloride is a selective antagonist of both α-adrenoceptor and calmodulin that is commonly used for the treatment of hypertension, specifically caused by pheochromocytoma. The IC50 (100 nM) derived from the blockade of [3H]yohimbine binding by phenoxybenzamine was significantly less than the IC50 (550 nM) for the corresponding reversal by phenoxybenzamine of the effects of norepinephrine on cyclic AMP accumulation[2]. Phenoxybenzamine hydrochloride (50 nM) in conbination with Phenoxybenzamine hydrochloridetolamine (1000 nM) enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with pretreatment with Phenoxybenzamine hydrochloride (50 nM) alone in endothelium-intact aortae. Combined treatment with either dexmedetomidine (300 or 1000 nM) and Phenoxybenzamine hydrochloride (50 nM) or Phenoxybenzamine hydrochloridetolamine (1000 nM) and Phenoxybenzamine hydrochloride (50 nM) enhance Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with Phenoxybenzamine hydrochloride alone (50 nM)[3]. PHEN (Phenoxybenzamine Hydrochloride) exhibited a significant inhibitory effect on the proliferation of both U251 and U87MG glioma cell lines in a positive dose-dependent manner. PHEN apparently attenuated the malignancy of glioma in terms of migration and invasion and also suppressed the tumorigenic capacity both in vitro and in vivo[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03176693 Pheochromocytoma ... 展开 >> Paraganglioma 收起 << Phase 3 Recruiting May 2024 United States, California ... 展开 >> University of California, Los angeles Recruiting Los Angeles, California, United States, 90025 Principal Investigator: Masha J Livhits, MD          Sub-Investigator: Eric J Kuo, MD 收起 <<
NCT00569855 - Completed - -
NCT00569855 Open-heart Surgery ... 展开 >> Cardiopulmonary Bypass 收起 << Phase 2 Completed - United States, Arkansas ... 展开 >> Arkansas Children's Hospital Little Rock, Arkansas, United States, 72207 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.69mL

2.94mL

1.47mL

29.39mL

5.88mL

2.94mL
参考文献

[1]Byon HJ, Ok SH, et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenoceptor Blockade and Nitric Oxide Release in Isolated Rat Aortae. Int J Med Sci. 2017 Feb 7;14(2):143-149.

[2]Lenox RH, Ellis J, Van Riper D, Ehrlich YH. Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve. Mol Pharmacol. 1985;27(1):1-9

[3]Byon HJ, Ok SH, Lee SH, et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenoceptor Blockade and Nitric Oxide Release in Isolated Rat Aortae. Int J Med Sci. 2017;14(2):143-149. Published 2017 Feb 7

[4]Lin XB, Jiang L, Ding MH, et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016;37(3):2901-2908