product name Rilmenidine Phosphate
Description: Rilmenidine Phosphate, the water soluble form of Rilmenidine, is a selective I (1) imidazoline receptor agonist used for the treatment of hypertension. In Hep G2 cells treated with 0.5 mM oleic acid for 6 hours and 1μm Rilmenidine for 30 minutes, the oleic acid-induced lipid accumulation decreases. Stimulation of imidazoline I-1 receptor by Rilmenidine activated P38 to induce the expression of FXR. Mice fed with HFD (high fat diet) had improved hepatic steatosis following the administration of Rilmenidien through the activation of imidazoline I-1 receptor.
References: Am J Hypertens. 1992 Apr;5(4 Pt 2):99S-105S; Annu Rev Pharmacol Toxicol. 1996;36:511-44.
219.24
Formula
C12H11NO3
CAS No.
521937-07-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 43 mg/mL (196.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Rilmenidine phosphate is the water soluble form of Rilmenidine. It is an antihypertensive drug targets the imidazoline receptor. Kinase Assay: Cell Assay: In Hep G2 cells treated with 0.5 mM oleic acid for 6 hours and 1μm Rilmenidine for 30 minutes, the oleic acid-induced lipid accumulation decreases. Stimulation of imidazoline I-1 receptor by Rilmenidine activated P38 to induce the expression of FXR. |
|---|---|
| In Vivo | Mice fed with HFD (high fat diet) had improved hepatic steatosis following the administration of Rilmenidien through the activation of imidazoline I-1 receptor. Imidazoline receptors are involved in the bulbospinal regulation of blood pressure and affect peripheral stimulation. In hypertensive patients, Rilmenidine decreased blood pressure in a dose-dependent mater. In contrast with placebo, Rilmenidine had significantly lowered blood pressures. In addition, Rilmenidine had significantly less incidences of adverse effects than using other drugs for hypertension. |
| Animal model | |
| Formulation & Dosage | |
| References | Am J Hypertens. 1992 Apr;5(4 Pt 2):99S-105S; Annu Rev Pharmacol Toxicol. 1996;36:511-44; Cardiovasc Hematol Agents Med Chem. 2006 Jan;4(1):17-32; Naunyn Schmiedebergs Arch Pharmacol. 2012 Jan;385(1):51-6. |
