1-[3-[3-(4-氯苯基)丙氧基]丙基]哌啶盐酸盐
Pitolisant hydrochloride(1-[3-[3-(4-Chlorophenyl)propoxy]propyl]-piperidinehydrochloride)
CAS: 903576-44-3
化学式: C17H26ClNO.HCl
| 中文名 | Pitolisant hydrochloride |
| 英文名 | 1-[3-[3-(4-Chlorophenyl)propoxy]propyl]-piperidinehydrochloride |
| 别名 | 替洛利生盐酸盐 CIPROXIDINE 替洛利生 1-[3-[3-(4-氯苯基)丙氧基]丙基]哌啶盐酸盐 1-[3-[3-(4-氯丙基)丙氧基]丙基]-哌啶盐酸盐 |
| 英文别名 | BF 2649 PITOLISANT Ciproxidine Ciproxidine BF2649 CIPROXIDINE BF2649 Pitolisant hydrochloride Pitolisant (hydrochloride) 1-[3-[3-(4-Chlorophenyl)propoxy]propyl]-piperidinehydrochloride 1-[3-[3-(4-Chlorophenyl)propoxy]propyl]piperidine monohydrochloride Piperidine, 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-, hydrochloride |
| CAS | 903576-44-3 |
| 化学式 | C17H26ClNO.HCl |
| 分子量 | 332 |
| 存储条件 | Desiccate at RT |
| 体外研究 | On the stimulation of guanosine 5′-O-(3-[ 35 S]thio)triphosphate binding to this receptor, Pitolisant (BF2.649) behaves as a competitive antagonist with a K i value of 0.16 nM and as an inverse agonist with an EC 50 value of 1.5 nM and an intrinsic activity ~50% higher than that of ciproxifan. Pitolisant displaces [ 125 I]iodoproxyfan binding from mouse brain cortical membranes with an IC 50 value of 26.4±4.5 nM. Taking into account the K d value of the radioligand (161±9 pM), the deduced K i value for Pitolisant is 14±1 nM. Pitolisant displaces [ 125 I]iodoproxyfan binding from membranes of rat glioma C6 cells stably expressing the human H 3 receptor with an IC 50 value of 4.2±0.2 nM. Taking into account the K d value of the radioligand (50±4 pM), the deduced K i value for Pitolisant is 2.7±0.5 nM. Pitolisant progressively reverses this response with a Hill coefficient close to unity and an IC 50 value of 330±68 nM, leading to a K i value of 17±4 nM. Pitolisant elicits a dose-dependent decrease of the basal-specific [ 35 S]GTPγS binding to membranes with a maximal effect corresponding to 75±1% of the basal-specific binding and an EC 50 value of 1.5±0.1 nM. |
| 体内研究 | The administration of Pitolisantat a single dose of 10 mg/kg 30 min before a single dose of LY170053 (2 mg/kg b.w.) also significantly affects immobility time in the FST. Subsequent administration of the aforementioned drug sequence in mice statistically significantly increases the duration of immobility in comparison to the time determined in the control group in the FST. It decreased locomotor activity as well. In contrast, the results obtained in subchronic treatment after fifteen administrations of both drugs (Pitolisant 10 mg/kg b.w., and after 30 min LY170053 2 mg/kg b.w., and again after 4 h LY170053 2 mg/kg b.w.) show that the administration of Pitolisant followed by that of LY170053 equalized the locomotor activity in mice; in comparison to the level of motility in the control group, to which only Pitolisant is administered. More importantly, this combination of drugs significantly reduces immobility time to the level obtained in the control group in the forced swim test in mice [one-way ANOVA; F (3,20) =4.226,P=0.0181]. Rats given Pitolisant (10 mg/kg) during the conditioning phase stayed 502±94 s on the paired texture, a value not statistically different from that of controls, indicating that Pitolisant did not support place preference. |
1-[3-[3-(4-氯苯基)丙氧基]丙基]哌啶盐酸盐 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.012 ml | 15.06 ml | 30.12 ml |
| 5 mM | 0.602 ml | 3.012 ml | 6.024 ml |
| 10 mM | 0.301 ml | 1.506 ml | 3.012 ml |
| 5 mM | 0.06 ml | 0.301 ml | 0.602 ml |
最后更新：2024-01-02 23:10:35
![1-[3-[3-(4-氯苯基)丙氧基]丙基]哌啶盐酸盐](http://res.chembk.com/assets/images/structure/903576-44-3.gif)
供应商列表
主打产品现货供应
产品名: Pitolisant hydrochloride 去供应商网站查看 询盘CAS: 903576-44-3
产地: 上海
规格: 99%
价格: 10mg 840,50mg 3700,100mg 6000
库存: 现货
电话: 18301782025
手机: 18301782025
电子邮件: 3008007403@qq.com
QQ: 3008007403
微信: 18301782025
产品描述: Pitolisant hydrochloride 99% MedMol 货号：S87162
现货供应
产品名: Pitolisant hydrochloride 去供应商网站查看 询盘CAS: 903576-44-3
产地: 上海
规格: P876468
价格: 10mg-530,50mg-2355,1ml-588
库存: 7天内发货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
主打产品现货供应
产品名: Pitolisant hydrochloride 去供应商网站查看 询盘CAS: 903576-44-3
产地: 上海
规格: 99%
价格: 10mg 840,50mg 3700,100mg 6000
库存: 现货
电话: 18301782025
手机: 18301782025
电子邮件: 3008007403@qq.com
QQ: 3008007403
微信: 18301782025
产品描述: Pitolisant hydrochloride 99% MedMol 货号：S87162
现货供应
产品名: Pitolisant hydrochloride 去供应商网站查看 询盘CAS: 903576-44-3
产地: 上海
规格: P876468
价格: 10mg-530,50mg-2355,1ml-588
库存: 7天内发货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
您刚刚浏览过
你知道吗？
微信搜索化工百科或扫描下方二维码，添加化工百科小程序，随时随地查信息！