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| 品牌 | absin | CAS | 65-28-1 |
|---|---|---|---|
| 分子式 | C17H19N3O.CH4O3S | 纯度 | ＞98% |
| 分子量 | 377.46 | 货号 | abs47027598 |
| 规格 | 50mg | 供货周期 | 现货 |
| 主要用途 | used in the treatment of hypertension | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Phentolamine mesilate 65-28-1
| 产品描述 | |
| 描述 | Phentolamine mesylate is a nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 甲磺suan酚妥拉明 |
| 外观 | 白色或类白色结晶性粉末 |
| 可溶性/溶解性 | DMSO : 37.8 mg/mL (100 mM) water : 37.8 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | α-adrenergic receptor |
| In vitro(体外研究) | Phentolamine mesylate displaces binding of the selective alpha 1 receptor antagonists HEAT and prazosin and the alpha 2 receptor antagonists rauwolscine and RX 821002 with relatively high affinity in corpus cavernosum membranes. Phentolamine mesylate causes concentration dependent relaxation in erectile tissue strips pre-contracted with adrenergic agonists penylephrine, norepinephrine, oxymetazoline and UK 14,304, as well as with non-adrenergic contractile agents Endothelin and KCl. Phentolamine mesylate induces relaxation of corpus cavernosum erectile tissue by direct antagonism of alpha 1 and 2 adrenergic receptors and by indirect functional antagonism via a non-adrenergic, endothelium-mediated mechanism suggesting nitric oxide synthase activation. Phentolamine, an alpha-adrenergic antagonist, blocks the vasoconstriction associated with the epinephrine used in dental anesthetic formulations, thus enhancing the systemic absorption of the local anesthetic from the injection site. |
| In vivo(体内研究) | Phentolamine is a reversible competitive alpha-adrenergic antagonist with similar affinities for alphal and alpha2 receptors. Phentolamine mesylate causes vasodilatation and thus hypotension by decreasing peripheral vascular resistance. Phentolamine mesylate (30 and 100 nM) dose-dependently enhances electrical field stimulation-induced relaxation of the rabbit corpus cavernosum. Phentolamine relaxes rabbit corpus cavernosum independent of alpha-adrenergic receptor blockade. Phentolamine mesylate relaxes nonadrenergic noncholinergic neurons of the rabbit corpus cavernosum by activating NO synthase and is independent of alpha-adrenergic receptor blockade. |
| 参考文献 | |
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| 研究领域 | |
| 研究领域 | CancerCancer Metabolism CancerDrug resistance CancerTumor biomarkers NeuroscienceEndocrine system Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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