Alosetron (GR 68755) 是一种高效、高选择性的 5-HT3 受体 (5-HT3 receptor) 拮抗剂。Alosetron 用于肠易激综合征 (IBS) 的研究。Alosetron 阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化，IC50 在 ~55 nM。Alosetron 减轻清醒或麻醉犬直肠扩张的内脏伤害性效应。具有抗炎活性。
| 生物活性 |
Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects. |
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| 体内研究 |
Dexamethasone and Alosetron-treated (1 mg/kg; ip; daily for 6 days) rats exhibits a significant decrease in the diarrhea index, in comparison with TNBS-control group, especially after the initial 2 days of treatment following the induction of colitis.
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| 分子式 |
C17H18N4O
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| 分子量 |
294.35
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| CAS号 |
122852-42-0
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| 中文名称 |
阿洛司琼；洛曲尼斯；罗肠兴
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
| 临床试验 |
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