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.

Luc Maroteaux

Estelle Ayme-Dietrich

Gaëlle Aubertin-Kirch

Sophie Banas

Emily Quentin

Roland Lawson

Laurent Monassier

Alimentary Pharmacology & Therapeutics (Suppl)

Alimentary Pharmacology and Therapeutics, Supplement

New therapeutic opportunities for 5-HT2 receptor ligands

5-HT2受体配体的新治疗机会

New therapeutic opportunities for 5-HT2 receptor ligands

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