79944-58-4

Basic information

• Product Name: Idazoxan
• Synonyms: Idazoxan;IDAZOXAN,99%;2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole;dl-Idazoxan;2-(1-Imidazoline-2-yl)-2,3-dihydro-1,4-benzodioxin;2-(2-Imidazoline-2-yl)-2,3-dihydro-1,4-benzodioxin;Idezoxane;RX-781094
• CAS NO: 79944-58-4
• Molecular Formula: C₁₁H₁₂N₂O₂
• Molecular Weight: 204.23
• Mol File: 79944-58-4.mol
• Article Data: 8

Chemical Properties

• Boiling Point: 397 °C at 760 mmHg
• Flash Point: 193.9 °C
• Appearance: /
• Density: 1.39 g/cm³
• Vapor Pressure: 3.76E-06mmHg at 25°C
• Refractive Index: 1.665
• CAS DataBase Reference: Idazoxan(CAS DataBase Reference)
• NIST Chemistry Reference: Idazoxan(79944-58-4)
• EPA Substance Registry System: Idazoxan(79944-58-4)

Safety Data

• Hazardous Substances Data: 79944-58-4(Hazardous Substances Data)

Usage

Uses

alpha2-adrenergic blocker

Definition

ChEBI: A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group.

Metabolic pathway

When rats are administered radio-labeled idazoxan orally, the biotransformation of idazoxan is by hydroxylation at the 6- and 7-positions to form phenolic metabolites, which are excreted as glucuronide and sulfate metabolites in the urine, but unconjugated in the feces. Other minor metabolic pathways are 5-hydroxylation or oxidative degradation of the imidazoline ring, but these pathways are of quantitatively minor importance in rats.

InChI:InChI=1/C11H12N2O2/c1-2-4-9-8(3-1)14-7-10(15-9)11-12-5-6-13-11/h1-4,10H,5-7H2,(H,12,13)

Upstream product

• 92405-52-2 N-(2-aminoethyl)-2-(2-hydroxyphenoxy)-2-propenamide 
• 79944-55-1 ethyl (1,4-benzodioxan-2-yl)imidoate hydrochloride 
• 107-15-3 ethylenediamine 
• 1008-92-0 2-cyano-1,4-benzodioxane 
• 84687-14-9 (-)-Idazoxan 

Relevant articles and documents

THERAPY FOR COMPLICATIONS OF DIABETES

A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.

Method for treating resistant hypertension

A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Pharmaceutical composition based on idazoxan, salts, hydrates or polymorphs thereof

Pharmaceutical composition comprising 5 to 20% of an idazoxan salt or of idazoxan hydrate, 10 to 40% of microcrystalline cellulose, 1 to 5% of lubricant, 0.1 to 0.5% of colloidal silica and from 29.5% to 84.8% of lactose, with respect to the total mass.