PZ-1657 (Compound 57) is an orally active inverse agonist of the 5-HT7 receptor (5-HT7 receptor), with high selectivity, ability to penetrate the blood-brain barrier, and metabolic stability, demonstrating a Ki value of 5 nM. It effectively inhibits Gs pathway-mediated basal cyclic adenosine monophosphate (cAMP) production, with an EC50 value of 2.93 nM. Additionally, PZ-1657 inhibits CYP3A4P450 (IC50 = 12.2 μM) and affects the hERG channel. This compound also reduces MMP-9 activity mediated by the 5-HT7 receptor and reverses cognitive dysfunction induced by Phencyclidine. PZ-1657 exhibits antidepressant properties.