Serotonergic 5-HT₆ Receptor Antagonists: Heterocyclic Chemistry and Potential Therapeutic Significance

Title:Serotonergic 5-HT₆ Receptor Antagonists: Heterocyclic Chemistry and Potential Therapeutic Significance

Volume: 15 Issue: 17

Author(s): Alka Bali and Shalu Singh

Affiliation:

Keywords: 5-HT₆ antagonists, Alzheimer’s disease, Antiobesity agents, Cognition enhancers, Indole derivatives, Memory, Schizophrenia.

Abstract: The serotonin 5-HT₆ receptor (5- HT₆R) is amongst the recently discovered serotonergic receptors with almost exclusive localization in the brain. Hence, this receptor is fast emerging as a promising target for cognition enhancement in central nervous system (CNS) diseases such as Alzheimer’s disease (cognitive function), obesity, schizophrenia and anxiety. The last decade has seen a surge of literature reports on the functional role of this receptor in learning and memory processes and investigations related to the chemistry and pharmacology of 5-HT₆ receptor ligands, especially 5- HT₆ receptor antagonists. Studies show the involvement of multiple neurotransmitter systems in cognitive enhancement by 5-HT₆R antagonists including cholinergic, glutamatergic, and GABAergic systems. Several of the 5-HT₆R ligands are indole based agents bearing structural similarity to the endogenous neurotransmitter serotonin. Based on the pharmacophoric models proposed for these agents, drug designing has been carried out incorporating various heterocyclic replacements for the indole nucleus. In this review, we have broadly summarized the medicinal chemistry and current status of this fairly recent class of drugs along with their potential therapeutic applications.

Cite this article as:

Bali Alka and Singh Shalu, Serotonergic 5-HT₆ Receptor Antagonists: Heterocyclic Chemistry and Potential Therapeutic Significance, Current Topics in Medicinal Chemistry 2015; 15 (17) . https://dx.doi.org/10.2174/1568026615666150427110420