New therapeutic opportunities for 5-HT2 receptor ligands

Serotonergic dysfunction is mainly associated with neuropsychiatric and cardiovascular disorders but has also been linked with many other pathological conditions. Serotonin (5-hydroxytryptamine, 5-HT) mediates numerous physiological functions in the brain and the periphery by activating a variety of...

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Bibliographic Details
Published in:Pharmacology & therapeutics (Oxford) 2017-02, Vol.170, p.14-36
Main Authors: Maroteaux, Luc, Ayme-Dietrich, Estelle, Aubertin-Kirch, Gaëlle, Banas, Sophie, Quentin, Emily, Lawson, Roland, Monassier, Laurent
Format: Article
Language:English
Subjects:
Animal genetics
Animals
Biochemistry, Molecular Biology
Cardiology and cardiovascular system
Cardiovascular Diseases
Central Nervous System Diseases
Drug Design
Genetics
Human health and pathology
Humans
Life Sciences
Ligands
Molecular biology
Neoplasms
Neurobiology
Neurons and Cognition
Pharmaceutical sciences
Pharmacology
Psychiatrics and mental health
Pulmonology and respiratory tract
Receptors, Serotonin, 5-HT2
Serotonin
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Summary:Serotonergic dysfunction is mainly associated with neuropsychiatric and cardiovascular disorders but has also been linked with many other pathological conditions. Serotonin (5-hydroxytryptamine, 5-HT) mediates numerous physiological functions in the brain and the periphery by activating a variety of receptors. 5-HT receptors are divided into four classes, three of which belong to the G protein-coupled receptor family. This review provides an overview of the recent pharmacological developments involving the Gq-coupled 5-HT2 receptor subfamily as well as the pathological implications of this receptor subfamily with regard to fibrosis, the central nervous system, cardiovascular disorders, and cancer. The final section highlights new therapeutic opportunities and emerging research revealing unexplored medical opportunities for this class of 5-HT receptors. The development of biased 5-HT2 receptor ligands appears to be an interesting topic in various areas. In light of recent discoveries, the need for the development of new and safer drugs should take into account the risk of cardiovascular side effects such as pulmonary hypertension and heart valve disease.
ISSN:0163-7258
1879-016X
0163-7258
DOI:10.1016/j.pharmthera.2016.10.008