Current Topics in Medicinal Chemistry

Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc.
Doylestown, PA


Serotonin 5-HT6 Receptor Antagonists for the Treatment of Alzheimers Disease

Author(s): Werner J. Geldenhuys and Cornelis J. Van der Schyf

Affiliation: Department of Pharmaceutical Science, NEOUCOM, 4209 State Route 44, Rootstown,OH, 44272, USA.


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

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Article Details

Page: [1035 - 1048]
Pages: 14
DOI: 10.2174/156802608785161420
Price: $58