Identification | Back Directory | [Name]
Phentolamine mesilate | [CAS]
65-28-1 | [Synonyms]
REGITIN VASOMAX REGITIN MESYLATE regitinemesylate Phentolamine mesilat PHENTOLAMINE MESILATE PHENTOLAMINE MESYLATE regitinmethanesulphonate PHENTOLAMINEMESYLATE,USP Regitine methanesulfonate Phentolamine mesylate, >=99% PHENTOLAMINE METHANESULFONATE phentolaminemethanesulphonate Phentolamine Mesylate (200 mg) Phentolamine mesilate(Regitine) Phentolaminemethanesulfonate,99% Phentolamine·methanesulfonic acid PHENTOLAMINE METHANESULFONATE SALT PhentolamineMesylateCp2000/Usp26Gmp Phentolamine mesilate for system suitability PHENTOLAMINE METHANESULFONATE (PHENTOLAMINE MESYLATE) 3-[n-(2-imidazolin-2-ylmethyl)-p-toluidino]phenol methanesulphonate 2-[N-(M-HYDROXYPHENYL)-P-TOLUIDINOMETHYL]IMIDAZOLINE, METHANESULFONATE m-(n-(2-imidazolin-2-ylmethyl)-p-toluidino)-phenomonomethanesulfonate(sal 2-[N-(M-HYDROXYPHENYL)-P-TOLUIDINOMETHYL]IMIDAZOLIN METHANESULFONATE SALT 2-(N-[M-HYDROXYPHENYL]-P-TOLUIDINOMETHYL)IMIDAZOLINE METHANESULFONATE SALT 3-[[(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)METHYL](4-METHYLPHENYL)-AMINO]PHENOL MESYLATE 3-[4,5-Dihydro-1H-imidazol-2-ylmethyl-(4-methylphenyl)-amino]phenol methanesulfonate 3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]-phenol, methanesulfonate (1:1) 2-[N-(m-Hydroxyphenyl)-p-toluidinomethyl]imidazoline Methanesulfonate
Phentolamine Methanesulfonate PHENOL, 3-(((4,5-DIHYDRO-1H-IMIDAZOL-2-YL)METHYL)(4-METHYLPHENYL)AMINO)-, MONOMETHANESULFONATE (SALT) | [EINECS(EC#)]
200-604-6 | [Molecular Formula]
C18H23N3O4S | [MDL Number]
MFCD00134201 | [MOL File]
65-28-1.mol | [Molecular Weight]
377.46 |
Chemical Properties | Back Directory | [Appearance]
Crystalline Solid | [Melting point ]
180-182 °C(lit.)
| [density ]
1.2256 (rough estimate) | [refractive index ]
1.6320 (estimate) | [storage temp. ]
Refrigerator | [solubility ]
ethanol: 26 mg/mL
| [form ]
powder
| [color ]
white to off-white
| [Water Solubility ]
50 mg/mL | [Merck ]
14,7264 | [Stability:]
Aq. Solutions Cannot be Stored | [InChI]
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) | [InChIKey]
OGIYDFVHFQEFKQ-UHFFFAOYSA-N | [SMILES]
N(CC1=NCCN1)(C1C=CC(C)=CC=1)C1C=CC=C(O)C=1.S(=O)(=O)(O)C |
Hazard Information | Back Directory | [Chemical Properties]
Phentolamine mesylate (65-28-1) is a white, odourless powder which is soluble in water and alcohol. | [Uses]
An adrenergic blocking agent. An antihypertensive. Used for the treatment of pheochromocytoma. | [Uses]
Phentolamine Mesylate is a nonselective alpha-adrenergic antagonist with IC50 of 0.1 μM | [Brand name]
Regitine
(Novartis) [Name previously used: Phentolamine Methanesulfonate.]. | [General Description]
Phentolamine Mesylate(65-28-1) belongs to the class of alpha adrenergic antagonist drugs. It is used in the treatment of pheochromocytoma-related hypertension, erectile dysfunction and in the diagnosis of pheochromocytoma and norepinephrine-related dermal necrosis. | [Biochem/physiol Actions]
α-Adrenergic receptor antagonist; peripheral vasodilator. | [Clinical Use]
Alpha-adrenoceptor blocker:
Hypertensive crisis | [Safety Profile]
Poison by intravenous and subcutaneous routes. Experimental reproductive effects. When heated to decomposition it emits toxic fumes of SOx and NOx. | [Drug interactions]
Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Antidepressants: additive hypotensive effect with
MAOIs - avoid.
Antihypertensives: enhanced hypotensive effect.
Avanafil, vardenafil, sildenafil and tadalafil: enhanced
hypotensive effect - avoid concomitant use.
Diuretics: enhanced hypotensive effect.
Linezolid: additive hypotensive effect.
Moxisylyte: possibly severe postural hypotension. | [Metabolism]
Phentolamine is extensively metabolised.
Only about 10-13% of an intravenous dose is excreted
unchanged in the urine, and the fate of the remainder of
the drug is unknown. | [storage]
Store at +4°C | [Mode of action]
Phentolamine Mesylate is the mesylate salt of a synthetic imidazoline with alpha-adrenergic antagonist activity. As a competitive alpha-adrenergic antagonist, phentolamine binds to alpha-1 and alpha-2 receptors, resulting in a decrease in peripheral vascular resistance and vasodilatation. This agent also may block 5-hydroxytryptamine (5-HT) receptors and stimulate release of histamine from mast cells. |
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