| CAS NO: | 65-28-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 377.46 |
|---|---|
| Formula | C17H19N3O.CH4O3S |
| CAS No. | 65-28-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 76 mg/mL (201.3 mM) |
| Water: 76 mg/mL (201.3 mM) | |
| Ethanol: 76 mg/mL (201.3 mM) | |
| Other info | Chemical Name: 3-(((4,5-dihydro-1H-imidazol-2-yl)methyl)(p-tolyl)amino)phenol methanesulfonate InChi Key: OGIYDFVHFQEFKQ-UHFFFAOYSA-N InChi Code: InChI=1S/C17H19N3O.CH4O3S/c1-13-5-7-14(8-6-13)20(12-17-18-9-10-19-17)15-3-2-4-16(21)11-15;1-5(2,3)4/h2-8,11,21H,9-10,12H2,1H3,(H,18,19);1H3,(H,2,3,4) SMILES Code: CC1=CC=C(C=C1)N(CC2=NCCN2)C3=CC(=CC=C3)O.CS(=O)(=O)O |
| Synonyms | Phentolamine mesilate, Phentolamine methanesulfonate, OraVerse, Regitine mesylate, Regitine, Regityn, Rogitine, Z-Max, Phentolamine Mesylate, |
| In Vitro | In vitro activity: 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. 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 | 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Int J Impot Res. 1998 Dec;10(4):215-23; Fundam Clin Pharmacol. 2001 Feb;15(1):1-7. |
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