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LP-211

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产品介绍
产品介绍
产品信息
抗原名称
5-HT7 receptor;5-HT1A receptor;D2 receptor

商品描述
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).

分子量
466.62

纯度
98%

可溶性
DMSO : 100 mg/mL (214.31 mM; Need ultrasonic)
Ethanol : 50 mg/mL (107.15 mM; Need ultrasonic)
Ethanol : 50 mg/mL (107.15 mM; Need ultrasonic)

外观
clear white to light brown solid

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.

背景
分子式
C30H34N4O

CAS号
1052147-86-0

制备和贮存
保存方式
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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