Rilmenidine hemifumarate 是一种创新的抗压药和口服活性选择性 I1 咪唑啉受体 (I1 Imidazoline Receptor) 激动剂。Rilmenidine hemifumarate 也是一种α2肾上腺素受体激动剂。Rilmenidine phosphate 诱导Autophagy" style="display: inline; color: #c13a36">自噬 (Autophagy)。Rilmenidine hemifumarate 可通过减少交感神经过度活跃而发挥中枢作用，并通过抑制 Na+/H+反向转运而在肾脏中发挥作用。Rilmenidine hemifumarate可调节白血病细胞增殖，刺激促凋亡蛋白 Bax，从而诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。

Rilmenidine hemifumarate is an innovative antihypertensive agent that 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].

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) suppresses 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.

Rilmenidine-treated N171-82Q mice (i.p.; 4-times a week) shows 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].

207572-68-7

C14H20N2O5

238.28

Rilmenidine (hemifumarate)

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years