| 名称 | Phentolamine mesylate |
| 描述 | Phentolamine mesylate (Phentolamine methanesulfonate) is a nonselective alpha-adrenergic antagonist used to treat hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of [RAYNAUD DISEASE] and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. |
| 体外活性 | Phentolamine mesylate displaces binding of the selective alpha 1 receptor antagonists [125I]HEAT and [3H]prazosin and the alpha 2 receptor antagonists [3H]rauwolscine and [3H]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 phenylephrine, 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. [1] 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. [2] |
| 体内活性 | 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. [4] 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. [5] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 37.8 mg/mL (100 mM)
DMSO : 60 mg/mL (158.96 mM)
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| 关键字 | hypertension | Phentolamine mesylate | Beta Receptor | blood | vessels | pheochromocytoma | adrenergic | Phentolamine Mesylate | Adrenergic Receptor | erectile | vascular | Phentolamine | Inhibitor | failure | dysfunction | inhibit | resistance | heart | peripheral |
| 相关产品 | Octopamine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride |
| 相关库 | 经典已知活性库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 抑制剂库 | FDA 上市药物库 | GPCR靶点分子库 | 抗癌药物库 |
United States
