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Phenoxybenzamine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:63-92-3
包装与价格:
包装价格(元)
200 mg电议
500 mg电议
1 g电议
1 mL*10 mM(in DMSO)电议

产品名称
NCI-c01661
NSC 37448
Phenoxybenzamine HCl
盐酸酚苄明
产品介绍
Phenoxybenzamine hydrochloride 是一种选择性的 α-adrenoceptor 和 calmodulin 的抑制剂,是常用的抗高血压药。

产品描述

Phenoxybenzamine Hydrochloride 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

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[1]. 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[2].

体内活性

Phenoxybenzamine hydrochloride (20 nM, s.c.) effectively suppresses the tumorigenesis of glioma cells in mice and the cell density in Phenoxybenzamine hydrochloride-U87 mg xenografts decreases significantly[3]. Phenoxybenzamine hydrochloride (1 mg/kg, i.v.) treated rats shows significant improvements in NSS and foot fault scoring[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.

Cas No.

63-92-3

分子式

C18H23Cl2NO

分子量

340.3

别名

NCI-c01661;NSC 37448;Phenoxybenzamine HCl;盐酸酚苄明

储存和溶解度

H2O:14 mg/mL (41.1 mM)
Ethanol:63 mg/mL (185.1 mM)
DMSO:63 mg/mL (185.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years