LP-211

LP-211化学性质

沸点 :714.8±60.0 °C(Predicted)
密度 :1.17±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO:100.0(Max Conc. mg/mL);214.3(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);107.15(Max Conc. mM)
酸度系数(pKa) :15.39±0.46(Predicted)
形态 :solid
颜色 :clear white to light brown

LP-211性质、用途与生产工艺

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)

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.

LP-211上下游产品信息

上游原料

下游产品

LP-211 试剂级价格

LP-211生产厂家