54187-04-1

Basic information

• Product Name: Rilmenidine
• Synonyms: n-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine;oxaminozoline;RILMENIDINE;1,1-dicyclopropyl-n-(2-oxazolinyl)-methylamin;2-((dicyclopropylmethyl)imino)-oxazolidin;2-((dicyclopropylmethyl)imino)oxazolidine;2-(dicyclopropylmethylamino)-2-oxazoline;4,5-dihydro-n-(dicyclopropylmethyl)-2-oxazolamin
• CAS NO: 54187-04-1
• Molecular Formula: C₁₀H₁₆N₂O
• Molecular Weight: 180.25
• EINECS: 259-021-0
• Product Categories: Antihypertensive;Imidazoline binding site
• Mol File: 54187-04-1.mol
• Article Data: 1

Chemical Properties

• Melting Point: 106-107°
• Boiling Point: 355.469 °C at 760 mmHg
• Flash Point: 168.782 °C
• Appearance: white/solid
• Density: 1.455 g/cm³
• Vapor Pressure: 2.53E-27mmHg at 25°C
• Storage Temp.: Store at -20°C
• Solubility: H2O: 7.3 mg/mL
• PKA: 7.88±0.50(Predicted)
• CAS DataBase Reference: Rilmenidine(CAS DataBase Reference)
• NIST Chemistry Reference: Rilmenidine(54187-04-1)
• EPA Substance Registry System: Rilmenidine(54187-04-1)

Safety Data

• Safety Statements: 22-24/25
• WGK Germany: 3
• RTECS: RP7207400
• Hazardous Substances Data: 54187-04-1(Hazardous Substances Data)

Usage

Description

Rilmenidine is a new antihypertensive agent with a selective alphaz-agonist/antagonist profile, reportedly useful in the management of mild to moderate hypertension. Its fmt-line indication is possible because of the clear dissociation of its antihypertensive activity from other neurophannacological effects.

Chemical Properties

water soluble

Originator

Servier (France)

Uses

I1-imidazoline binding site ligand and a2-adrenoceptor agonist, exhibits higher I1 vs. a2 selectivity than clonidine

Brand name

Hyperium

Biological Activity

I 1 -imidazoline binding site selective ligand and α 2 -adrenoceptor agonist. Possesses greater I 1 vs α 2 selectivity than the prototypical compound, clonidine.

Metabolic pathway

In short-term rat hepatocyte cultures, oxaminozoline is metabolized and its four metabolites resulting from oxidation or hydrolysis are identified, three of which are identical to those reported in vivo. The presence of an additional minor metabolite in culture may be due to the higher metabolic rate of oxaminozoline in this model system.

InChI:InChI=1/2C10H16N2O.C4H4O4/c2*1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10;5-3(6)1-2-4(7)8/h2*7-9H,1-6H2,(H,11,12);1-2H,(H,5,6)(H,7,8)/b;;2-1+

Upstream product

• 54187-44-9 S 11460 
• 54187-03-0 1-(2-chloroethyl)-3-(dicyclopropylmethyl)urea 

Relevant articles and documents

Cyclopropylamines as pharmaceuticals

The present invention relates to cyclopropylmethyl amines substituted by a heterocyclic radical. More particularly the heterocyclic radical is a nitrogen containing ring with 5, 6 or 7 links interrupted by another hetero atom selected from the group consisting of oxygen, sulphur and imino--NH-- The invention also relates to the acid addition salts thereof with physiologically compatible mineral or organic acids. The invention extends to the processes for making them and the intermediates produced hereto. The invention also includes the pharmaceutical compositions incorporating as active ingredient at least one compound of the invention with an inert carrier. The compounds have therapeutic utility namely on the cardio-vascular diseases and on the neuro-psychological disturbances.