title: New therapeutic opportunities for 5-HT2receptor ligands.
abstract: 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-HT2receptor 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-HT2receptor 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.
authors: INSERM UMR S-839, Institut du Fer à Moulin, Université Pierre et Marie Curie, 17 rue du Fer à Moulin 75005, Paris, France.
authors: Luc
authors: L
authors: Maroteaux
authors: Laboratoire de Neurobiologie et Pharmacologie Cardiovasculaire EA7296, Faculté de Médecine, Fédération de Médecine Translationnelle de Strasbourg, Université et Centre Hospitalier de Strasbourg, Strasbourg, France.
authors: Estelle
authors: E
authors: Ayme-Dietrich
authors: Laboratoire de Neurobiologie et Pharmacologie Cardiovasculaire EA7296, Faculté de Médecine, Fédération de Médecine Translationnelle de Strasbourg, Université et Centre Hospitalier de Strasbourg, Strasbourg, France.
authors: Gaëlle
authors: G
authors: Aubertin-Kirch
authors: INSERM UMR S-839, Institut du Fer à Moulin, Université Pierre et Marie Curie, 17 rue du Fer à Moulin 75005, Paris, France.
authors: Sophie
authors: S
authors: Banas
authors: INSERM UMR S-839, Institut du Fer à Moulin, Université Pierre et Marie Curie, 17 rue du Fer à Moulin 75005, Paris, France.
authors: Emily
authors: E
authors: Quentin
authors: Laboratoire de Neurobiologie et Pharmacologie Cardiovasculaire EA7296, Faculté de Médecine, Fédération de Médecine Translationnelle de Strasbourg, Université et Centre Hospitalier de Strasbourg, Strasbourg, France.
authors: Roland
authors: R
authors: Lawson
authors: Laboratoire de Neurobiologie et Pharmacologie Cardiovasculaire EA7296, Faculté de Médecine, Fédération de Médecine Translationnelle de Strasbourg, Université et Centre Hospitalier de Strasbourg, Strasbourg, France. Electronic address: laurent.monassier@unistra.fr.
authors: Laurent
authors: L
authors: Monassier
mesh_terms: D000818:Animals; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000503:physiopathology; D002493:Central Nervous System Diseases / Q000188:drug therapy / Q000503:physiopathology; D015195:Drug Design; D006801:Humans; D008024:Ligands; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D044348:Receptors, Serotonin, 5-HT2 / Q000187:drug effects* / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism*
chemical_list: D008024:Ligands; D044348:Receptors, Serotonin, 5-HT2; D012701:Serotonin
keywords: 5-HT(2) receptors; Pathological function; Selectivity; Therapeutic track