Abstract

Recently, the serotonin 5-HT6 receptor has been identified as a drug target for attenuating cognitive deficits associated with Alzheimers disease (AD). Additionally, this receptor may also play a role in schizophrenia, anxiety and obesity. Reports in the literature suggest that the production of selective antagonists for the 5-HT6 receptor has increased during the last 10 years, with some compounds currently in clinical trials for the treatment of AD. In this review, we will address the rationale for using 5-HT6 receptor antagonists in AD, as well as report on current advances in the understanding of the structure-activity relationships required to synthesize 5-HT6 receptor antagonists.

Keywords: QSAR, G-coupled protein receptor, GCPR, tryptamine, arylsulfonyl, multifunctional, dementia