Aryl Biphenyl-3-ylmethylpiperazines as 5-HT7 Receptor Antagonists (pages 1855–1864)
Jeeyeon Kim, Youngjae Kim, Prof. Jinsung Tae, Miyoung Yeom, Prof. Bongjin Moon, Dr. Xi-Ping Huang, Prof. Bryan L. Roth, Kangho Lee, Dr. Hyewhon Rhim, Prof. Il Han Choo, Prof. Youhoon Chong, Dr. Gyochang Keum, Dr. Ghilsoo Nam and Prof. Hyunah Choo
Article first published online: 3 SEP 2013 | DOI: 10.1002/cmdc.201300240
Vacancies filled: 2′-Methoxybiphenyl-3-ylmethyl(2-methoxyphenyl)piperazine (28) is shown to serve as a selective 5-HT7 receptor antagonist. From a comparison with the docking modes of other known 5-HT7 receptor agonists and antagonists, it is suggested that occupancy of both hydrophobic ligand binding sites of the 5-HT7 receptor by the ligand is crucial for its antagonistic property.