LP-211，≥98% (HPLC)

LP-211 is a brain penetrant selective agonist for the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor. The 5-HT7 receptor is involved in a variety of central nervous system functions including circadian rhythm, sleep, thermoregulation, nociception, and memory, and appears to be involved in cognitive disorders, anxiety, and depression. LP-211 has been used as a selective 5-HT7 receptor agonist in multiple models including studies as a potential therapeutic agent in models of Rett syndrome and Fragile X Syndrome.

 

LP-211 是血清素 5-HT7 受体的脑渗透选择性激动剂，对大鼠克隆的 5-HT7 受体的 Ki 值为 0.58 nM，选择性超过 5-HT1A 受体的 300 倍。 5-HT7 受体参与多种中枢神经系统功能，包括昼夜节律、睡眠、体温调节、伤害感受和记忆，并且似乎与认知障碍、焦虑和抑郁有关。 LP-211 已在多种模型中用作选择性 5-HT7 受体激动剂，包括在雷特综合征和脆性 X 综合征模型中作为潜在治疗剂的研究。