中文名 | ASIMADOLINE |
英文名 | ASIMADOLINE |
别名 | 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 |
英文别名 | EMD61753 EMD-61753 EMD 61753 ASIMADOLINE Asimadoline (EMD-61753 N-((S)-2-((S)-3-Hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2,2-diphenylacetamide Benzeneacetamide, N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-α-phenyl- N-[(1S)-2-[(3S)-3-Hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-alpha-phenylbenzeneacetamide |
CAS | 153205-46-0 |
化学式 | C27H30N2O2 |
分子量 | 414.54 |
密度 | 1.170±0.06 g/cm3(Predicted) |
沸点 | 605.8±55.0 °C(Predicted) |
酸度系数 | 14.79±0.20(Predicted) |
存储条件 | 2-8°C |
体外研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.412 ml | 12.062 ml | 24.123 ml |
5 mM | 0.482 ml | 2.412 ml | 4.825 ml |
10 mM | 0.241 ml | 1.206 ml | 2.412 ml |
5 mM | 0.048 ml | 0.241 ml | 0.482 ml |
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