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- Phentolamine mesilate 65-28-1

- Phentolamine mesilate 65-28-1
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 receptorIn 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 参考文献 1. Giussani DA, et al. J Physiol. 1995 Jul 1;486 ( Pt 1):249-55.
2. Polak J, et al. Diabetologia. 2005 Dec;48(12):2631-40.
3. Trendelenburg AU, et al. Br J Pharmacol. 2003 Apr;138(8):1389-402.
研究领域 研究领域 CancerCancer MetabolismCancerDrug resistanceCancerTumor biomarkersNeuroscienceEndocrine systemDrug DiscoverySmall Molecule DrugLead Compound DiscoveryPhentolamine mesilate 65-28-1温馨提示:本产品仅作科研实验使用,不支持临床等研究
