Alvimopan monohydrate (ADL 8-2698 monohydrate) 是一种有效，选择性，具有口服活性和可逆的 μ-阿片受体 (μ-opioid receptor) 拮抗剂，IC50 值为 1.7 nM。Alvimopan monohydrate 对 μ-阿片受体 (Ki=0.47 nM) 的选择性高于 κ- (Ki=100 nM) 和 δ-阿片受体 (Ki=12 nM)。Alvimopan monohydrate 可用于术后肠梗阻的研究。
| 生物活性 |
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus. |
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| 体外研究 |
Alvimopan inhibits the loperamide-stimulated [S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 of 1.7 nM. |
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| 体内研究 |
Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of Sn-labelled microspheres produced by morphine in rats.
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| 分子式 |
C25H34N2O5
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| 分子量 |
442.55
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| CAS号 |
1383577-62-5
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| 中文名称 |
爱维莫潘水合物
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 临床试验 |
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纯度： 98%
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