The role of 5 HT6-receptor antagonists in Alzheimer's disease: an update.
Rita KhouryNoam GrysmanJake GoldKush PatelGeorge T GrossbergPublished in: Expert opinion on investigational drugs (2018)
Despite early positive findings, larger phase-III trials have failed to demonstrate any statistically significant impact on cognition for both idalopirdine and intepirdine, as adjunct to cholinesterase inhibitors. Paradoxically, 5-HT6 receptor agonists have also been shown to have cognitive enhancing properties. Thus, a better understanding of the mechanism of action of the 5-HT6 receptor and its ligands is warranted. Investigating 5-HT6 receptor partial or inverse agonists may be promising in future AD trials.