79944-58-4

Usage

Uses

Used in Pharmaceutical Industry:
Idazoxan is used as an alpha2-adrenergic blocker for the treatment of various medical conditions. It works by blocking the action of alpha2-adrenergic receptors, which play a role in regulating blood pressure, heart rate, and other physiological functions. By inhibiting these receptors, Idazoxan can help to lower blood pressure and improve cardiovascular function in patients with hypertension or other related conditions.
Additionally, Idazoxan has been studied for its potential use in treating other conditions, such as glaucoma, where it may help to reduce intraocular pressure, and in the management of certain psychiatric disorders, where it may help to modulate neurotransmitter activity in the brain. However, further research is needed to fully understand the therapeutic potential of Idazoxan in these areas.

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

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

Relevant academic research and scientific papers

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.

ANTIHYPERTENSIVE THERAPY

A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective 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. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.

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

A pharmaceutical composition comprising idazoxan or derivatives and their therapeutically acceptable salts, racemates, optically active isomers and polymorphs.

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.

Benzodioxane-imidazoline compounds as antihypertensives

Compounds of the formula STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein: n is an integer equal to 0, 1, 2 or 3; R1 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl lower alkyl; each R is independently hydrogen, lower alkyl, optionally substituted phenyl, or optionally substituted phenyl lower alkyl; are α2 blockers, and, therefore, are useful in treating essential hypertension and depression, and in inhibiting platelet aggregation.

An Investigation of Some Base Induced Transformations of The 1,4-Benzodioxan Ring System

The reaction between benzodioxan-2-carboxylic acid and ethylenediamine has been examined and related base induced transformations investigated.

α-Adrenoreceptor reagents. I. Synthesis of some 1,4-benzodioxans as selective presynaptic α2-adrenoreceptor antagonists and potential antidepressants

The rational design of RX 781094, 2-(1,4-benzodioxan-2-yl)-2-imidazoline hydrochloride (5), a new potent and selective antagonist of α2-adrenoreceptors, is discussed. A compound that acts as an antagonist at presynaptic α2-adrenoreceptors could be an effective and novel treatment of depression because of its ability to increase the concentration of norepinephrine at central receptor sites. The effects of substituents in the aromatic and imidazoline rings have been examined, as well as the replacement of the imidazoline ring by an amidine function or by other heterocyclic ring systems. None of these derivatives are as potent or selective as 5, although some do display a degree of selectivity as antagonists. Some derivatives were found to possess agonist properties that, with the exception of 23, favored the postsynaptic site. Compounds 9, 12, 16, 21, 30, and 51 possessing presynaptic α2-adrenoreceptor antagonist and postsynaptic α1-adrenoreceptor partial agonist properties were also obtained, and these derivatives could be considered as potential antimigraine agents.