LP-211

中文名称:

LP-211

中文同义词:

英文名称:

N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide

英文同义词:

LP-211;N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide;LP-211; LP 211; LP211;1052147-86-0;LP21;LP-211 >=98% (HPLC)

CAS号:

1052147-86-0

分子式:

C30H34N4O

分子量:

466.62

EINECS号:

相关类别:

API

Mol文件:

1052147-86-0.mol

储存条件 

2-8°C

形态

solid

颜色

clear white to light brown

生物活性

LP-211 是一种选择性的，可透过血脑屏障的 5-HT7 受体激动剂，Ki 值为 0.58 nM，选择性高于 5-HT1A 受体 (Ki，188 nM) 和 D2 受体 (Ki，142 nM)。

靶点

5-HT 7 Receptor 0.58 nM (Ki) 5-HT 1A Receptor 188 nM (Ki) D 2 Receptor 142 nM (Ki)

5-HT 7 Receptor 0.58 nM (Ki)

5-HT 1A Receptor 188 nM (Ki)

体外研究

LP-211 is a selective 5-HT 7 receptor agonist, with a K i of 0.58 nM, 324- and 245-fold selectivity over 5-HT 1A receptor (K i , 188 nM) and D 2 receptor (K i , 142 nM). LP-211 shows agonist properties with an EC 50 of 0.6 μM.

体内研究

LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean C max of 0.76 ± 0.32 μg/mL at 30 min. 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. 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.