L-803087 是一种有效的选择性的生长抑素 sst4 受体激动剂，Ki 为 0.7 nM，比其他生长抑素受体的选择性高 280 倍以上。L-803087 在体外促进 AMPA 介导的海马突触反应，在体内增加了海藻酸盐诱导的小鼠癫痫发作。
| 生物活性 |
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice. |
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| IC50&Target |
Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor) |
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| 体外研究 |
L-803087 has Ki values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively. |
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| 体内研究 |
L-803087 (5 nmol) is doubled seizure activity in wild-type mice on average. Interestingly, this effect is blocked by 3 nmol Octreotide. In hippocampal slices from wild-type mice, Octreotide (2 μM) does not modify AMPA-mediated synaptic responses while facilitation occurred with L-803087 (2 μM).
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| 分子式 |
C25H29F2N5O3
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| 分子量 |
485.53
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| CAS号 |
217480-26-7
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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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纯度： 98%
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