米贝地尔
中文名称 | 米贝地尔 |
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中文同义词 | 米贝地尔;米贝地尔(二盐酸盐);CALCIUM CHANNEL抑制剂(MIBEFRADIL DIHYDROCHLORIDE);咪拉地尔 |
英文名称 | MIBEFRADIL DIHYDROCHLORIDE |
英文同义词 | C07222;(1S,2S)-2-[2-[[3-(1H-Benzimidazol-2yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenylmethoxyacetoacetatedihydrochloride;Acetic acid, Methoxy-, 2-[2-[[3-(1H-benziMidazol-2-yl)propyl]MethylaMino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-Methylethyl)-2-naphthalenylester, (1S-cis)-;(1S,2S)-2-[2-[[3-(2-Benzimidazolyl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl methoxyacetate;(1S,2S)-2-[2-[[3-(1H-BENZIMIDAZOL-2YL)PROPYL]METHYLAMINO]ETHYL]-6-FLUORO-1,2,3,4-TETRAHYDRO-1-(1-METHYLETHYL)-2-NAPHTHALENYL METHOXYACETOACETATE DIHYDROCHLORIDE;(1S,2S)-2-[2[[3-(2-BENZIMIDAZOLYLPROPYL]METHYLAMINO]ETHYL]-6-FLUORO-1,2,3,4-TETRAHYDRO-1-ISOPROPYL-2-NAPHTHYL METHOXYACETATE DIHYDROCHLORIDE;RO 40-5967;MIBEFRADIL DIHYDROCHLORIDE |
CAS号 | 116644-53-2 |
分子式 | C29H38FN3O3 |
分子量 | 495.63 |
EINECS号 | |
相关类别 | 膜转运/离子通道;细胞生物学试剂 |
Mol文件 | 116644-53-2.mol |
结构式 |
米贝地尔 性质
熔点 | 125 - 130°C |
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沸点 | 647.6±55.0 °C(Predicted) |
密度 | 1.18±0.1 g/cm3(Predicted) |
储存条件 | Desiccate at RT |
溶解度 | 可溶于DMSO(少许)、甲醇(少许) |
酸度系数(pKa) | 11.93±0.10(Predicted) |
形态 | 固体 |
颜色 | 米白色 |
IC50: 2.7 μM (T-type calcium channel), 18.6 μM (L-type calcium channel)
Mibefradil 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 differed 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 Ethosuximide show significant lower Ca V 3.2 expression in the spinal cord and DRG.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-15553A | Mibefradil dihydrochloride | 1 mg | 340元 | |
2024/01/25 | HY-15553A | 米贝地尔 Mibefradil dihydrochloride | 116644-53-2 | 5mg | 850元 |