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Phentolamine mesylate

Phentolamine mesylate (Phentolamine methanesulfonate) 是一种非选择性的、可逆的，具有口服活性的 α1 和 α2 肾上腺素能受体阻滞剂，能够扩张使血管，降低周围血管阻力。它可用于研究嗜铬细胞瘤相关的高血压，心力衰竭和勃起功能障碍。

CAS号

65-28-1

分子式

C17H19N3O·CH4O3S

主要靶点

Adrenergic Receptor

仅限科研使用

Cat No : CM02562

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Synonyms

Phentolamine mesilate|Phentolamine methanesulfonate|甲磺酸酚妥拉明

验证数据展示

  • CAS No.: 65-28-1

    Phentolamine mesylate
    CAS#: 65-28-1

产品信息

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.

CAS号 65-28-1
分子式 C17H19N3O·CH4O3S
主要靶点 Adrenergic Receptor
主要通路 G蛋白偶联受体|神经科学
分子量 377.46
纯度 99.77%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Phentolamine mesilate|Phentolamine methanesulfonate|甲磺酸酚妥拉明

靶点活性

α-adrenoceptor:5 - 30 nM

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]

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]

溶解度

DMSO:37.8 mg/mL (100 mM),H2O:37.8 mg/mL (100 mM)

参考文献

1.Traish A, et al. Int J Impot Res,1998, 10(4), 215-223.
2.Moore PA, et al. Anesth Prog,2008, 55(2), 40-48.
3.Holt A, et al. J Pharm Pharmacol,1995, 47(10), 837-845.
4.Vemulapalli S, et al. Fundam Clin Pharmacol,2001, 15(1), 1-7.

The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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