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Phentolamine methanesulfonate

Phentolamine methanesulfonate structure

CAS No:
65-28-1
Formula:
C17H19N3O.CH4O3S
Chemical Name:
Phentolamine methanesulfonate
Synonyms:
Phenol,3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]-,methanesulfonate (1:1);Phenol,m-[N-(2-imidazolin-2-ylmethyl)-p-toluidino]-,monomethanesulfonate (salt);Phenol,3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]-,monomethanesulfonate (salt);m-[N-(2-Imidazolin-2-ylmethyl)-p-toluidino]phenol methanesulfonate;Phentolamine mesylate;Phentolamine methanesulfonate;Regitine methanesulfonate;Regitin methanesulphonate;Phentolamine methanesulphonate;Regitine mesylate;Vasomax;Rogitine;252228-09-4
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Phentolamine mesylate is a competitive, reversible α-adrenoceptor antagonist with an IC50 between 5 and 30 nM.

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.|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.

Phentolamine methanesulfonate Basic Attributes

Molecular Weight：

377.46

Exact Mass：

377.140930

EC Number：

200-604-6

UNII：

Y7543E5K9T

DSSTox ID：

DTXSID60215315

NCI Thesaurus Code：

C38691

HScode：

2933290090

Characteristics

PSA：

111

Appearance：

white to off-white powder

Density：

1.2256 (rough estimate)

Melting Point：

177-181 °C

Boiling Point：

551°C at 760 mmHg

Flash Point：

287ºC

Water Solubility：

H2O: 50 mg/mL;ethanol: 26 mg/mL

Storage Conditions：

Refrigerator

Toxicity：

LDLo scu-rat: 275 mg/kg NIIRDN 6,667,82

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

wgk germany：

hazard class code：

20/21/22-36/37/38

safety instructions：

26-36

RTECS Number：

SL5430000

Marks：

Xn,Xi

Stability/Shelf Life：

Aq. Solutions Cannot be Stored

Precautionary statement(s)：

P261-P280-P305 + P351 + P338

Hazard Statements：

H302 + H312 + H332-H315-H319-H335

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P312, P321, P322, P330, P332+P313, P337+P313, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 42 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma. (See all compounds classified as Adrenergic alpha-Antagonists.)

MeSH Entry Terms：

Fentolamin

Phentolamine methanesulfonate Use and Manufacturing

Uses

An adrenergic blocking agent.An antihypertensive.Used for the treatment of pheochromocytoma.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:377.5
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:4
Exact Mass:377.14092740
Monoisotopic Mass:377.14092740
Topological Polar Surface Area:111
Heavy Atom Count:26
Complexity:456
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Short-acting non-selective α-receptor blockers (α1, α2) can antagonize the effects of adrenaline and norepinephrine in the blood circulation, causing vasodilation and reducing peripheral vascular resistance; they antagonize the effects of catecholamines and are used to diagnose and treat pheochromocytoma, but have little effect on the blood pressure of normal people or patients with essential hypertension; they can reduce peripheral vascular resistance, reduce cardiac afterload, decrease left ventricular end-diastolic pressure and pulmonary artery pressure, and increase cardiac output, and can be used to treat heart failure.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Phentolamine Mesylate for Injection
Ingredients	The main component and chemical name of this product are: 3[(4,5-dihydro-1-imidazol-2-yl)methyl](4-methylphenyl)aminophenol methanesulfonate. Molecular formula: C17H19N3OCH4O3S, molecular weight: 377.46.
Indication	1. When used in combination with sympathomimetic amines, the latter's peripheral vasoconstriction effect is offset or weakened; 2. When used in combination with guanethidine, the incidence of orthostatic hypotension or tachycardia is high; 3. When used in combination with diazoxide, the effect of diazoxide in inhibiting insulin release is inhibited.
Specifications	10mg
Manufacturer	Shanghai Fudan Fuhua Pharmaceutical Co., Ltd.

Phentolamine Mesylate for Injection
Ingredients	The main ingredients of this product and their chemical names are: The main ingredient is: Phentolamine mesylate, and its chemical name is: 3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]phenol mesylate.
Indication	1. When used in combination with sympathomimetic amines, the latter's peripheral vasoconstriction effect is offset or weakened; 2. When used in combination with guanethidine, the incidence of orthostatic hypotension or bradycardia increases; 3. When used in combination with diazoxide, the inhibitory effect of diazoxide on insulin release is inhibited; 4. Sedative hypnotics such as phenobarbital and doxepin and antihypertensive drugs such as reserpine and jiangyaling can enhance the antihypertensive effect of this product; 5. When used in combination with cardiac glycosides, its toxic reactions can be enhanced; 6. Avoid use with iron preparations; 7. This product cannot be used in combination with nitroglycerin drugs.
Specifications	10mg
Manufacturer	Hainan Poly Pharm. Co., Ltd.

Phentolamine Mesylate for Injection
Ingredients	The main ingredients of this product and their chemical names are: The main ingredient is: Phentolamine mesylate, and its chemical name is: 3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]phenol mesylate.
Indication	1. When used in combination with sympathomimetic amines, the latter's peripheral vasoconstriction effect is offset or weakened; 2. When used in combination with guanethidine, the incidence of orthostatic hypotension or bradycardia increases; 3. When used in combination with diazoxide, the inhibitory effect of diazoxide on insulin release is inhibited; 4. Sedative hypnotics such as phenobarbital and doxepin and antihypertensive drugs such as reserpine and jiangyaling can enhance the antihypertensive effect of this product; 5. When used in combination with cardiac glycosides, its toxic reactions can be enhanced; 6. Avoid use with iron preparations; 7. This product cannot be used in combination with nitroglycerin drugs.
Specifications	10 mg

See More Related Drugs

Registered Holders

MATRIX PHARMACORP PRIVATE LTD

United States
Active
RELIABLE BIOPHARMACEUTICAL LLC

United States
Active
China Resources Double-Crane Pharmaceutical Co., Ltd.

China
Active

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Guide of Phentolamine methanesulfonate

Description
Basic Attributes
Characteristics
Safety Information
Drug Information
Use and Manufacturing
Computed Properties
Drug Function and Efficacy
Related Drugs
Registered Holders
Recommended Suppliers
Latest News
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