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Phentolamine Mesylate
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。
Phentolamine Mesylate图片
CAS NO:65-28-1
包装与价格:
包装价格(元)
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
甲磺酸酚妥拉明
Phentolamine mesilate
Phentolamine methanesulfonate
产品介绍
Phentolamine mesylate 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。

产品描述

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.

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]

Cas No.

65-28-1

分子式

C18H23N3O4S

分子量

377.46

别名

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

储存和溶解度

H2O:37.8 mg/mL (100 mM)
DMSO:37.8 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years