Idalopirdine (Lu AE58054 ) 是有效，选择性的5-HT6受体拮抗剂，Ki为 0.83 nM。Idalopirdine 可用于阿尔茨海默病和精神分裂症等相关疾病的研究。
| 生物活性 | Idalopirdine (Lu AE58054 ) is a potent, selective5-HT6 receptorantagonist with aKivalue of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders[1][2]. |
| IC50& Target | 5-HT6Receptor 0.83 nM (Ki) |
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体内研究
(In Vivo) | Idalopirdine (intraperitoneal injection, 5 mg/kg, daily, 28 days) can reduce food intake and body weight in over-eating rat models[1].
Idalopirdine (1 or 2 mg/kg, i.v) can dose-dependently increase the gamma power during nPO electrical stimulation, enhance effect of donepezil on cortical gamma oscillations but no alteration of sleep-wake patterns in rats[2].
| Animal Model: | Male Wistar rats[1] | | Dosage: | 5 mg/kg | | Administration: | intraperitoneal injection, daily, 28 days | | Result: | Significantly reduced the amount of calories consumed by animals in a palatable diet and significantly reduced plasma levels of glucose, triglycerides and cholesterol. |
| Animal Model: | Male Sprague-Dawley rats[2] | | Dosage: | 1 or 2 mg/kg | | Administration: | i.v. | | Result: | No significant increase in the gamma power at 1 mg/kg and significantly increased the gamma power at 2 mg/kg.
Significantly enhanced and/or prolonged effect of low-dose donepezil (0.3 mg/kg) on gamma power during 60-minute nPO stimulation after donepezil administration. |
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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. |
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