LP-211

LP-211CAS号: 1052147-86-0分子式: C30H34N4O分子量: 466.62描述纯度储存/保存方法外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
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).
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
外观
clear white to light brown solid
可溶性/溶解性
DMSO : 100 mg/mL (214.31 mM; Need ultrasonic)
Ethanol : 50 mg/mL (107.15 mM; Need ultrasonic)
生物活性
靶点
5-HT7 receptor;5-HT1A receptor;D2 receptor
In vitro(体外研究)
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.
In vivo(体内研究)
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. 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.

分子结构图

LP-211