CAS 207572-68-7|Rilmenidine hemifumarate
| Common Name | Rilmenidine hemifumarate | ||
|---|---|---|---|
| CAS Number | 207572-68-7 | Molecular Weight | 476.566 |
| Density | / | Boiling Point | / |
| Molecular Formula | C24H36N4O6 | Melting Point | / |
| MSDS | USA | Flash Point | / |
Names
| Name | Rilmenidine hemifumarate salt |
|---|---|
| Synonym | More Synonyms |
Rilmenidine hemifumarate BiologicalActivity
| Description | Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells [1][2][3]. |
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| Related Catalog | Signaling Pathways >>Neuronal Signaling >>Imidazoline ReceptorSignaling Pathways >>Apoptosis >>ApoptosisResearch Areas >>CancerResearch Areas >>Cardiovascular DiseaseSignaling Pathways >>GPCR/G Protein >>Imidazoline ReceptorSignaling Pathways >>Autophagy >>AutophagySignaling Pathways >>GPCR/G Protein >>Adrenergic Receptor |
| In Vitro | Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors[1]. Rilmenidine (25-100 μM; 24 hours) inhibits K562 cell proliferation[2]. Cell Viability Assay[2] Cell Line: K562 cells Concentration: 25, 50, 100 μM Incubation Time: 24 hours Result: Dose-dependently inhibited K562 colony formation. |
| In Vivo | Rilmenidine-treated N171-82Q mice (i.p.; 4-times a week) displays significant improved forelimb grip strength and all limbs grip strength from 12 to 22 weeks of age[3]. Rilmenidine decreases levels of mutant huntingtin[3]. |
| References | [1]. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S. [2]. Srdic-Rajic T, et al. Rilmenidine suppresses proliferation and promotes apoptosis via the mitochondrial pathway in human leukemic K562 cells. Eur J Pharm Sci. 2016;81:172-180. [3]. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S. [4]. Rose C, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease. Hum Mol Genet. 2010;19(11):2144-2153. |
Chemical & Physical Properties
| Molecular Formula | C24H36N4O6 |
|---|---|
| Molecular Weight | 476.566 |
| Exact Mass | 476.263489 |
| InChIKey | LZFATBMLSYHRTC-WXXKFALUSA-N |
| SMILES | C1COC(NC(C2CC2)C2CC2)=N1.C1COC(NC(C2CC2)C2CC2)=N1.O=C(O)C=CC(=O)O |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| Safety Phrases | S22;S24/25 |
| RIDADR | NONH for all modes of transport |
| RTECS | RP7207400 |
Articles3
More Articles| The involvement of pertussis toxin-sensitive G proteins in the post receptor mechanism of central I1-imidazoline receptors. Br. J. Pharmacol. 120 , 1575, (1997) 1. To elucidate the possible involvement of pertussis toxin (PTX)-sensitive G proteins in the post receptor mechanism of alpha 2-adrenoceptors and imidazoline receptors, we examined the effect of pret... | |
| Role of imidazoline receptors in the cardiovascular actions of moxonidine, rilmenidine and clonidine in conscious rabbits. J. Pharmacol. Exp. Ther. 276 , 411, (1998) The present study in conscious rabbits with intracisternal (i.c.) catheters sought to determine the relative contribution of the I1 subtype of imidazoline receptors (IR) and alpha 2 adrenoceptors to t... | |
| Rilmenidine elevates cytosolic free calcium concentration in suspended cerebral astrocytes. J. Neurochem. 71 , 1429-1435, (1998) Rilmenidine, a ligand for imidazoline and alpha2-adrenergic receptors, is neuroprotective following focal cerebral ischemia. We investigated the effects of rilmenidine on cytosolic free Ca2+ concentra... |
Synonyms
| N-(Dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine (2E)-but-2-enedioate (2:1) |
| MFCD00673925 |
| N-(Dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine (2E)-2-butenedioate (2:1) |
| 2-Oxazolamine, N-(dicyclopropylmethyl)-4,5-dihydro-, (2E)-2-butenedioate (2:1) |
| MFCD09878261 |
