207572-68-7
中文名稱
RILMENIDINE HEMIFUMARATE SALT
英文名稱
RILMENIDINE HEMIFUMARATE SALT
CAS
207572-68-7
分子式
2C10H16N2O.C4H4O4
分子量
476.57
MOL 文件
207572-68-7.mol
207572-68-7 結(jié)構(gòu)式
基本信息
中文別名
化合物 T21911 英文別名
LZFATBMLSYHRTC-WXXKFALUSA-NRILMENIDINE HEMIFUMARATE SALT
n-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine hemifumarate salt
Oxaminozoline hemifumarate salt, Rilmenidene hemifumarate salt, N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine hemifumarate salt
常見問題列表
生物活性
Rilmenidine hemifumarate 是一種新型的抗高血壓藥物和口服活性選擇性 I1 咪唑啉受體 (I1 imidazoline receptor) 激動劑。Rilmenidine hemifumarate 也是一種 α2 腎上腺素受體激動劑。Rilmenidine phosphate 誘導(dǎo)自噬 (autophagy)。Rilmenidine hemifumarate 可通過減少交感神經(jīng)過度活躍而發(fā)揮中樞作用，并通過抑制 Na+/H+ 反向轉(zhuǎn)運而在腎臟中發(fā)揮作用。Rilmenidine hemifumarate可調(diào)節(jié)白血病細胞增殖，刺激促凋亡蛋白 Bax，從而誘導(dǎo)人白血病 K562 細胞線粒體通路的紊亂和凋亡。體外研究
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. |
體內(nèi)研究
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.