LP-211

别名

6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid 4-cyano-benzylamide,N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide,N-[(4-Cyanophenyl)methyl]-4-[1,1′-biphenyl]-2-yl-1-piperazinehexanamide

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.