Bioactivity | Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine 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]. |
Invitro | 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: |
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]. |
Name | Rilmenidine |
CAS | 54187-04-1 |
Formula | C10H16N2O |
Molar Mass | 180.25 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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]. 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. |