Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Phentolamine mesylate (Phentolamine methanesulfonate) 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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
100 mg | In stock | $ 51.00 | |
200 mg | In stock | $ 67.00 | |
500 mg | In stock | $ 153.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 50.00 |
Description | Phentolamine mesylate (Phentolamine methanesulfonate) 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. |
Targets&IC50 | α-adrenoceptor:5 - 30 nM |
In vitro | 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] |
In vivo | 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] |
Synonyms | Phentolamine methanesulfonate, Phentolamine mesilate |
Molecular Weight | 377.46 |
Formula | C17H19N3O·CH4O3S |
CAS No. | 65-28-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 37.8 mg/mL (100 mM)
DMSO: 37.8 mg/mL (100 mM)
You can also refer to dose conversion for different animals. More
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Phentolamine mesylate 65-28-1 GPCR/G Protein Neuroscience Adrenergic Receptor Phentolamine methanesulfonate hypertension Beta Receptor blood vessels pheochromocytoma adrenergic Phentolamine Mesylate erectile vascular Phentolamine Inhibitor failure dysfunction inhibit resistance heart peripheral Phentolamine mesilate inhibitor