65-28-1 Usage
Description
Phentolamine mesilate, also known as Regitine, is a nonselective alpha-adrenergic antagonist with an IC50 of 0.1 μM. It is a white crystalline powder that is soluble in water and has a molecular formula of C16H19N3O?CH4O3S. Phentolamine mesilate is a derivative of imidazoline and belongs to the class of adrenergic blocking agents.
Uses
Used in Pharmaceutical Industry:
Phentolamine mesilate is used as an adrenergic blocking agent and an antihypertensive for the treatment of pheochromocytoma, a rare tumor of the adrenal gland that produces excessive amounts of catecholamines, leading to high blood pressure and other symptoms.
Used in Clinical Settings:
Phentolamine mesilate is used as a diagnostic tool in the evaluation of suspected pheochromocytoma. It can help to confirm the diagnosis by causing a drop in blood pressure when administered to patients with this condition.
Used in Emergency Medicine:
Phentolamine mesilate can be used in emergency situations to treat hypertensive crisis, particularly in cases of drug-induced hypertension or severe hypertension due to other causes.
Used in Research:
Phentolamine mesilate is used in research settings to study the effects of alpha-adrenergic receptors and their role in various physiological processes, such as blood pressure regulation, neurotransmission, and smooth muscle contraction.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 65-28-1 includes 5 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 2 digits, 6 and 5 respectively; the second part has 2 digits, 2 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 65-28:
(4*6)+(3*5)+(2*2)+(1*8)=51
51 % 10 = 1
So 65-28-1 is a valid CAS Registry Number.
InChI:InChI=1/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)
65-28-1Relevant articles and documents
Process for synthesis of phentolamine mesylate (by machine translation)
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Paragraph 033; 0034; 0035; 0036, (2016/10/07)
The invention discloses a synthesis process of phentolamine mesilate. The synthesis process of the phentolamine mesilate comprises the following steps: A, neutralizing, namely, adjusting phentolamine hydrochloride by using diluted ammonia water for many times under the action of silica gel until proper pH value is achieved, and filtering to obtain filtrate to obtain phentolamine free alkali, watering and washing with distilled water for many times until the filtrate is qualified through chloride tracking detection, and drying and crystallizing to obtain a phentolamine free alkali refined product; and B, salifying namely, adding an ethanol solution of methanesulfonic acid into the phentolamine free alkali refined product dropwise by taking absolute ethanol as a solvent, precisely adjusting the pH value to be 5 to 6, then performing a water bath vacuum distillation salt forming reaction, inoculating ethyl acetate, separating out and crystallizing, washing and drying to obtain the phentolamine mesilate. According to the synthesis process of the phentolamine mesilate, the prominent problems that chloride and pH value are not easy to control during actual production are solved, purity is high and impurities are few.