5-HT₆ Receptor Modulator

5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pK_i of 6.33 (5-HT6) and a pIC₅₀ valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC₅₀ = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

1-(1-Naphthyl)piperazine is a 5-HT receptor modulator that acts as both a 5-HT2A receptor antagonist and 5-HT1A receptor agonist, and binds to human 5-HT6 receptor with a K_i of 120 nM. 1-(1-Naphthyl)piperazine partially inhibits forskolin-stimulated adenylate cyclase activity in calf substantia nigra. 1-(1-Naphthyl)piperazine inhibits UV-induced immunosuppression. 1-(1-Naphthyl)piperazine induces S-phase cell cycle delay, apoptosis and increases ROS levels, leading to inhibit MNT-1 cell proliferation. 1-(1-Naphthyl)piperazine can be used for melanoma research.

Goxalapladib is a 5-HT₆ receptor modulator that blocks lipoprotein-associated phospholipase A2 (Lp-PLA2) activity. Goxalapladib is promising for research of atherosclerosis-associated cardiovascular diseases.