| CAS |
No.1052147-86-0 |
| 英文名称 |
LP-211 |
| 别名 |
N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide |
| 分子式 |
C30H34N4O |
| 分子量 |
466.62 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
Light yellow to yellow Oil |
| 储存条件 |
Store at -20℃，2 years |
| SMILES |
C1CN(CCN1CCCCCC(=O)NCC2=CC=C(C=C2)C#N)C3=CC=CC=C3C4=CC=CC=C4 |
| 靶点 |
5-HT Receptor |
| 通路 |
Neuronal Signaling;GPCR & G Protein |
| 背景说明 |
LP-211是一种选择性的 5-HT7 受体激动剂。 |
| 生物活性 |
LP-211 is a selective and blood?brain barrier penetrant 5-HT7 receptor agonist， with a Ki of 0.58 nM， with high selectivity over 5-HT1A receptor (Ki， 188 nM) and D2 receptor (Ki， 142 nM).[1-3] |
| In Vitro |
LP-211 is a selective 5-HT7 receptor agonist， with a Ki of 0.58 nM， 324- and 245-fold selectivity over 5-HT1A receptor (Ki， 188 nM) and D2 receptor (Ki， 142 nM). LP-211 shows agonist properties with an EC50 of 0.6 μM[1]. |
| In Vivo |
LP-211 (10 mg/kg， i.p.) rapidly reaches the systemic circulation in the mouse， with mean Cmax of 0.76 ± 0.32 μg/mL at 30 min[1]. LP-211 (0.003-0.3 mg/kg， i.p.) significantly increases the micturition volume in a dose-dependent manner， and causes significant increases in voiding efficiency in spinal cord-injured (SCI) rats， and such effects can be completely reversed by SB-269970[2]. LP-211 (0.25 and 0.50 mg/kg i.p.) improves consolidation of chamber-shape memory in rats， resulting in significant novelty-induced hyperactivity and recognition[3]. |
| 动物实验 |
Thirty male adult Wistar rats (300-450 g) are assessed for novelty preference behavior after acute treatment (administered immediately after the training session and 24 h before the test session). After a 4 weeks wash out， the rPDT is conducted to evaluate attraction from a greater/uncertain reward， with a sub-chronic treatment (five injections， immediately after sessions which follow the indifferent point). Food restriction， imposed by the experimenter through a limited quantity of food given at the end of each rPDT session， is applied to increase motivation to work for food delivery. All behavioral tests take place between 9:30 am and 4:00 pm. Rats are randomly assigned to treatment (LP-211 at 0.25 or 0.50 mg/kg i.p.) and control groups (injection volume 10 mL/kg; n?=?10 per group). The brain penetrant 5-HT7R agonist LP-211 is dissolved in a vehicle solution of 1% dimethyl sulfoxide (DMSO) in saline (0.9% NaCl). Control group receives the vehicle strictly in the same conditions[3]. |
| 激酶实验 |
Binding of [3H]-LSD at rat cloned 5-HT7 receptor is performed in the assay. In 1 mL of incubation buffer (50 mM Tris， 10 mM MgCl2 and 0.5 mM EDTA， pH 7.4) are suspended 30 μg of membranes， 2.5 nM [3H]-LSD， LP-211 (6?9 concentrations). The samples are incubated for 60 min at 37°C. The incubation is stopped by rapid filtration on GF/A glass fiber filters (presoaked in 0.5% polyethylenimine for 30 min). The filters are washed with 3 × 53 mL of ice-cold buffer (50 mM Tris， pH 7.4). Nonspecific binding is determined in the presence of 10 μM 5-CT. Approximately 90% of specific binding is determined under these conditions[1]. |
| 数据来源文献 |
[1]. Leopoldo M， et al. Structural modifications of N-(1，2，3，4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. J Med Chem. 2008 Sep 25;51(18):5813-22.
[2]. Norouzi-Javidan A， et al. Effect of 5-HT7 receptor agonist， LP-211， on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33. eCollection 2016.
[3]. Beaudet G， et al. LP-211， a selective 5-HT7 receptor agonist， increases novelty-preference and promotes risk-prone behavior in rats. Synapse. 2017 Dec;71(12). |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号