Karila_2015_J.Med.Chem_58_7901

Reference

Title : Therapeutic Potential of 5-HT6 Receptor Agonists - Karila_2015_J.Med.Chem_58_7901
Author(s) : Karila D , Freret T , Bouet V , Boulouard M , Dallemagne P , Rochais C
Ref : Journal of Medicinal Chemistry , 58 :7901 , 2015
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.

PubMedSearch : Karila_2015_J.Med.Chem_58_7901
PubMedID: 26099069

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Citations formats

Karila D, Freret T, Bouet V, Boulouard M, Dallemagne P, Rochais C (2015)
Therapeutic Potential of 5-HT6 Receptor Agonists
Journal of Medicinal Chemistry 58 :7901

Karila D, Freret T, Bouet V, Boulouard M, Dallemagne P, Rochais C (2015)
Journal of Medicinal Chemistry 58 :7901