S 3341-3
Rilmenidine
CAS: 54187-04-1
Molecular Formula: C10H16N2O
S 3341-3 - Names and Identifiers
| Name | Rilmenidine |
| Synonyms | S 3341-3 RILMENIDINE Rilmenidine fumaric acid oxaminozoline 2-(dicyclopropylmethylamino)-2-oxazoline 2-((dicyclopropylmethyl)imino)-oxazolidin 2-((dicyclopropylmethyl)imino)oxazolidine 2-[N-(Dicyclopropylmethyl)amino]oxazoline 1,1-dicyclopropyl-n-(2-oxazolinyl)-methylamin 4,5-dihydro-n-(dicyclopropylmethyl)-2-oxazolamin N-(dicyclopropylmethyl)-4,5-dihydrooxazol-2-amine N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine n-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine N-(Dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine |
| CAS | 54187-04-1 |
| EINECS | 259-021-0 |
| 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+ |
S 3341-3 - Physico-chemical Properties
| Molecular Formula | C10H16N2O |
| Molar Mass | 180.25 |
| Density | 1.45±0.1 g/cm3(Predicted) |
| Melting Point | 106-107° |
| Boling Point | 355.5±9.0 °C(Predicted) |
| Flash Point | 431.1°C |
| Solubility | H2O: 7.3mg/mL |
| Vapor Presure | 2.53E-27mmHg at 25°C |
| Appearance | solid |
| Color | white |
| pKa | 7.88±0.50(Predicted) |
| Storage Condition | Store at -20°C |
| Physical and Chemical Properties | Crystallized from hexane, melting point 106~107 ℃. Rimenidine phosphate (Rilmenidine Phosphate):C10H16N2O?H3PO4. PKa 9.3. Solubility in water: about 19% W/V; Solubility in methanol: about 7% W/V; Solubility in chloroform and ethanol: 0.7% W/V. Acute toxic LD50 mice, rats (mg/kg):375,295 oral. |
| In vitro study | Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors. Rilmenidine (25-100 μM; 24 hours) inhibits K562 cell proliferation. Cell Viability Assay Cell Line: K562 cells Concentration: 25, 50, 100 μM Incubation Time: 24 hours Result: Dose-dependently inhibited K562 colony formation. |
| In vivo study | 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. Rilmenidine decreases levels of mutant huntingtin. |
S 3341-3 - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | RP7207400 |
S 3341-3 - Reference Information
| biological activity | Rilmenidine is a new type of antihypertensive drug and oral active selective I1 imidazoline receptor (I1 imidazoline receptor) agonist. Rilmenidine is an α2 adrenoceptor agonist. Rilmenidine induces autophagy (autophagy). Rilmenidine can play a central role by reducing sympathetic hyperactivity and in the kidney by inhibiting Na +/H + reverse transport. Rilmenidine can regulate the proliferation of leukemia cells and stimulate the pro-apoptotic protein Bax, thus inducing mitochondrial pathway disorder and apoptosis in human leukemia K562 cells. |
| in vitro study | Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors. Rilmenidine (25-100 μ m; 24 hours) inhibits K562 cell proliferation. Cell Viability Assay Cell Line: K562 cells Concentration: 25, 50,100 μ m Incubation Time: 24 hours result: dose-dependently inhibited K562 colony formation. |
| Cell Line: | K562 cells |
| Concentration: | 25, 50, 100 μM |
| Incubation Time: | 24 hours |
| Result: | Dose-dependently inhibited K562 colony formation. |
| in vivo study | 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. Rilmenidine decreases levels of huntingtin. |
| chemical properties | crystallized from hexane with a melting point of 106~107 ℃. Rimenidine phosphate (Rilmenidine Phosphate):C10H16N2O?H3PO4. PKa 9.3. Solubility in water: about 19% W/V; Solubility in methanol: about 7% W/V; Solubility in chloroform and ethanol: 0.7% W/V. Acute toxic LD50 mice, rats (mg/kg):375,295 oral. |
| use | oxazoline antihypertensive drugs. There is no sedative effect under the usual dose, and there is no obvious adverse effect on blood sugar, blood lipid and renal function. For hypertension. |
| production method | method 1: compound (I) reacts with phenyl chloroformate to obtain compound (II). (II) Reaction with Aminoethanol to Produce Compound (III). (Ⅲ) Chlorinated with dichlorosulfoxide to obtain compound (Ⅳ). (IV) Cyclic is delimenidine. Method 2: Compound (I) and chloroethyl isocyanate act directly to obtain compound (IV). Re-ring delimenidine. |
Last Update：2024-04-09 18:58:34
