Phenoxybenzamine hydrochloride,63-92-3

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YZ剂描述：

产品名称：Phenoxybenzamine hydrochloride

产品别名：盐酸酚苄明

英文别名：Phenoxybenzamine hydrochloride

靶点：CAM；α-adrenergic receptor

CAS：63-92-3

纯度：0.99

外观：白色或类白色结晶性粉末

保存方法：Store at -20°C

描述：

Phenoxybenzamine hydrochloride is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM. It is used as an anti-hypertensive due to its efficacy in reducing the vasoconstriction caused by adrenaline and noradrenaline. Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. It remains permanently bound to the receptor, preventing adrenaline and noradrenaline from binding. This causes vasodilatation in blood vessels, due to its antagonistic effect at the alpha-1 adrenoceptor found in the walls of blood vessels, resulting in a drop in blood pressure.?

溶解性：Ethanol ：63 mg/mL (185.1 mM)
DMSO ：63 mg/mL (185.1 mM)
Water ：14 mg/mL (41.1 mM)

体外研究：

The IC50 (100 nM) derived from the blockade of [3H]yohimbine binding by Phenoxybenzamine hydrochloride is significantly less than the IC50 (550 nM) for the corresponding reversal by Phenoxybenzamine hydrochloride of the effects of norepinephrine on cyclic AMP accumulation. 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). In addition, combined treatment with Phenoxybenzamine hydrochloridetolamine and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride combined treatment. ​Combined treatment with high concentrations of dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with combined treatment with low concentrations of dexmedetomidine (300 nM) and Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride (0.1-100 μM) inhibits glioma proliferation, migration, and invasion and suppresses the tumorigenesis capacity. Phenoxybenzamine hydrochloride also inhibits self-renewal of glioma stem-like cells. Phenoxybenzamine hydrochloride activates LINGO-1 and inhibits the TrkB-Akt pathway. Phenoxybenzamine hydrochloride (0.1 μM-1 mM) preserves primary neurons within the CA1, CA3 and dentate gyrus and produces a robust neuroprotective effect, and prevents neuronal death from OGD in all regions of the hippocampus when delivered at 2, 4, and 8 h post-OGD at 100 μM.

体内研究：Phenoxybenzamine hydrochloride (20 nM, s.c.) effectively suppresses the tumorigenesis of glioma cells in mice and the cell density in Phenoxybenzamine hydrochloride-U87MG xenografts decreases significantly. Phenoxybenzamine hydrochloride (1 mg/kg, i.v.) treated rats shows significant improvements in NSS and foot fault scoring.

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