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J Med Chem. 2015 Oct 22;58(20):7901-12. doi: 10.1021/acs.jmedchem.5b00179. Epub 2015 Jul 2.

Therapeutic Potential of 5-HT6 Receptor Agonists.

Author information

1
UNICAEN, CERMN (Centre d'Etudes et de Recherche sur le Médicament de Normandie), Université de Caen Basse-Normandie , F-14032 Caen, France.
2
UNICAEN, GMPc (Groupe Mémoire et Plasticité Comportementale), Université de Caen Basse-Normandie , F-14032 Caen, France.

Abstract

Given its predominant expression in the central nervous system (CNS), 5-hydroxytryptamine (5-HT: serotonin) subtype 6 receptor (5-HT6R) has been considered as a valuable target for the development of CNS drugs with limited side effects. After 2 decades of intense research, numerous selective ligands have been developed to target this receptor; this holds potential interest for the treatment of neuropathological disorders. In fact, some agents (mainly antagonists) are currently undergoing clinical trial. More recently, a series of potent and selective agonists have been developed, and preclinical studies have been conducted that suggest the therapeutic interest of 5-HT6R agonists. This review details the medicinal chemistry of these agonists, highlights their activities, and discusses their potential for treating cognitive issues associated with Alzheimer's disease (AD), depression, or obesity. Surprisingly, some studies have shown that both 5-HT6R agonists and antagonists exert similar procognitive activities. This article summarizes the hypotheses that could explain this paradox.

PMID:
26099069
DOI:
10.1021/acs.jmedchem.5b00179
[Indexed for MEDLINE]

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