生化/生理作用
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。
属性
溶解性
DMSO: 5 mg/mL, clear (warmed)
SMILES string
O=C(NCC1=CC=C(C#N)C=C1)CCCCCN2CCN(C3=CC=CC=C3C4=CC=CC=C4)CC2
InChI
1S/C30H34N4O/c31-23-25-14-16-26(17-15-25)24-32-30(35)13-5-2-8-18-33-19-21-34(22-20-33)29-12-7-6-11-28(29)27-9-3-1-4-10-27/h1,3-4,6-7,9-12,14-17H,2,5,8,13,18-22,24H2,(H,32,35)
InChI key
BQEDZLDNNBDKDS-UHFFFAOYSA-N