5-HT7 receptor antagonists generated antidepressant-like effects in animal model and the involvement of the 5-HT7 receptor in other pathophysiological mechanisms such as thermoregulation, learning and memory, and sleep has been highlighted by various studies. As one of our efforts to discover a new type of 5-HT7 receptor antagonists, we here report on the synthesis and binding affinities to the 5-HT7 receptor of the quinazolinone library 1, ...