米贝拉地尔
| 中文名称 | 米贝拉地尔 |
|---|---|
| 中文同义词 | 米贝拉地尔;米贝拉地尔二盐酸盐;盐酸米贝拉地尔;盐酸米贝地尔;(1S,2S)-2-(2-((3-(1H-苯并[D]咪唑-2-基)丙基)(甲基)氨基)乙基)-6-氟-1-异丙基-1,2,3,4-四氢萘-2-基 2-甲氧基乙酸酯 二盐酸盐;MIBEFRADILDIHYDROCHLORIDEHYDRATE>=98%(HPLC),POWDER;米贝拉地尔 二盐酸盐 水合物 |
| 英文名称 | MIBEFRADIL |
| 英文同义词 | [(1S,2S)-2-[2-[3-(1H-benzimidazol-2-yl)propyl-methyl-amino]ethyl]-6-fluoro-1-isopropyl-tetralin-2-yl] 2-methoxyacetate dihydrochloride;MIBEFRADIL;Mibefradil diHCl;(1S,2S)-2-[2[[3-(2-Benzimidazolyl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl methoxyacetate dihydrochloride hydrate;(1s-cis)-orid;2-(2-((3-(1h-benzimidazol-2-yl)propyl)methylamino)ethyl)-aceticaci;6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenylester,dihydrochl;ro40-5967/001 |
| CAS号 | 116666-63-8 |
| 分子式 | C29H40Cl2FN3O3 |
| 分子量 | 568.5506032 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 116666-63-8.mol |
| 结构式 |  |
米贝拉地尔 性质
| 熔点 | 128℃ |
|---|---|
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
| 溶解度 | H2O：24 mg/mL，可溶 |
| 酸度系数(pKa) | 4.8; 5.5(at 25℃) |
| 形态 | 固体 |
| 颜色 | 白色 |
| 稳定性 | 吸湿性 |
IC50: 2.7 μM (T-type calcium channel), 18.6 μM (L-type calcium channel)
Mibefradil dihydrochloride inhibits reversibly the T- and L-type currents with IC 50 values of 2.7 and 18.6 μM, respectively. The inhibition of the L-type current is voltage-dependent, whereas that of the T-type current is not. Ro 40-5967 blocks T-type current already at a holding potential of -100 mV At a higher concentration (20 µM), Mibefradil reduces the amplitude of excitatory junction potentials (by 37±10 %), slows the rate of repolarisation (by 44±16 %) and causes a significant membrane potential depolarisation (from −83±1 mV to −71±5 mV). At a higher Mibefradil concentration (20 µM) there is significant membrane potential depolarisation and a slowing of repolarisation. These actions of Mibefradil are consistent with K + channel inhibition, which has been shown to occur in human myoblasts and other cells.
The hearing thresholds of the 24-26 week old C57BL/6J mice differ following the 4-week treatment period. The hearing threshold at 24 kHz is significantly decreased in the Mibefradil-treated and benidipine-treated groups compared with the saline-treated group (P<0.05). Compared with the saline-treated group, rats receiving Mibefradil or NSC 64013 show significant lower Ca V 3.2 expression in the spinal cord and DRG.
安全信息
| WGK Germany | 3 |
|---|---|
| RTECS号 | AI8977250 |
| 毒性 | LD50 in mice, rats (mg/kg): 35, 23 i.v.; >800, >800 orally (Clozel) |