| 生物活性 | |||
|---|---|---|---|
| 描述 | As one of the nine members of the ClC family, ClC-2 (chloride channel type-2) is broadly expressed throughout the body, including the gastrointestinal tract [6]. Lubiprostone, a possible ClC-2 channel opener indicated for the treatment of constipation, increases chloride ion transport and fluid secretion into the intestinal lumen. Lubiprostone (3 nM–10 μM) induced a concentration-dependent contraction of the longitudinal muscle, with a pEC50 of 7.0 and maximal effect of 95±3% of the response to 1 μM PGE2 (n=4). Lubiprostone also caused a concentration-dependent contraction of circular muscle preparations. In rat colon longitudinal muscle, lubiprostone (10 nM–10 μM) caused a muscle contraction (maximum at 10 μM; 140±74% of the response to 1 μM PGE2, n=4). In human proximal stomach longitudinal muscle, lubiprostone induced a concentration-dependent contraction with a pEC50 of 6.4±0.2 and maximal effect at 10 μM of 102±17% of the response to 1 μM PGE2 (n=3) [7]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00953017 | - | Completed | - | - | |
| NCT03720613 | - | Not yet recruiting | November 1, 2025 | - | |
| NCT00577499 | - | Terminated(Recruitment was sub... 展开 >>optimal) 收起 << | - | - | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.56mL 0.51mL 0.26mL |
12.81mL 2.56mL 1.28mL |
25.61mL 5.12mL 2.56mL |
| 参考文献 |
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