阿西马朵林
| 中文名称 | 阿西马朵林 |
|---|---|
| 中文同义词 | 阿西马朵林;N-((S)-2-((S)-3-羟基吡咯烷-1-基)-1-苯乙基)-N-甲基-2,2-二苯基乙酰胺 |
| 英文名称 | ASIMADOLINE |
| 英文同义词 | ASIMADOLINE;N-[(1S)-2-[(3S)-3-Hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-alpha-phenylbenzeneacetamide;EMD 61753;Asimadoline (EMD-61753;Benzeneacetamide, N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-α-phenyl-;N-((S)-2-((S)-3-Hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2,2-diphenylacetamide;EMD-61753;EMD61753;EMD 61753 |
| CAS号 | 153205-46-0 |
| 分子式 | C27H30N2O2 |
| 分子量 | 414.54 |
| EINECS号 | |
| 相关类别 | Pharmaceutical intermediate |
| Mol文件 | 153205-46-0.mol |
| 结构式 |  |
阿西马朵林 性质
| 沸点 | 605.8±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.170±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：103mg/mL |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 14.79±0.20(Predicted) |
IC50: 5.6 nM (guinea pig κ opioid), 1.2 nM (human recombinant κ opioid)
Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC
50
for Asimadoline binding to μ-opioid receptors is 3 µM and to δ-opioid receptors is 0.7 µM. The IC
50
values for D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA and kainate/AMPA receptors are all >10 µM.
Asimadoline has affinity to sodium and L type Ca
2+
ion channels at IC
50
concentrations 150 to 800 fold the IC
50
for the κ receptors.
At high concentrations, Asimadoline demonstrates spasmolytic action against 400 µM barium chloride in the rat duodenum (IC
50
=4.2 µM), suggesting that Asimadoline may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.
Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.
The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels.
Treatment with Asimadoline (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes.
| Animal Model: | Adult female Sprague-Dawley rats |
| Dosage: | 1, 5, 15 mg/kg |
| Administration: | SC; single dose |
| Result: | Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-107384 | 阿西马朵林 Asimadoline | 153205-46-0 | 5mg | 950元 |
| 2024/01/25 | HY-107384 | 阿西马朵林 Asimadoline | 153205-46-0 | 10mg | 1750元 |