| 产品描述: | Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine Hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders |
| 靶点: |
5-HT6 Receptor:0.83 nM (Ki) |
| 体内研究: |
Idalopirdine (intraperitoneal injection, 5 mg/kg, daily, 28 days) Hydrochloride can reduce food intake and body weight in over-eating rat models. Idalopirdine (1 or 2 mg/kg, i.v) Hydrochloride 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. Animal Model: Male Wistar rats 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 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. |
| 参考文献: |
1. Magdalena Kotańska, et al. Idalopirdine, a selective 5-HT6 receptor antagonist, reduces food intake and body weight in a model of excessive eating. Metab Brain Dis. 2018 Jun;33(3):733-740. 2. Maria Amat-Foraster, et al. The 5-HT6 receptor antagonist idalopirdine potentiates the effects of donepezil on gamma oscillations in the frontal cortex of anesthetized and awake rats without affecting sleep-wake architecture. Neuropharmacology. 2017 Feb;113(Pt A):45-59. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.51 ml |
12.551 ml |
25.102 ml |
| 5 mM |
0.502 ml |
2.51 ml |
5.02 ml |
| 10 mM |
0.251 ml |
1.255 ml |
2.51 ml |
| 50 mM |
0.05 ml |
0.251 ml |
0.502 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |