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 [2].In Vitro: 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[2].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.
Rilmenidine decreases levels of mutant huntingtin.