title: 5-HT(1A) receptor: an old target as a new attractive tool in drug discovery from central nervous system to cancer.
abstract: The serotonin receptor subtype 5-HT(1A) was one of the first serotonin receptor subtypes pharmacologically characterized. This receptor subtype has long been object of intense research and is implicated in the pathogenesis and treatment of anxiety and depressive disorders. In recent years, new chemical entities targeting the 5-HT(1A) receptor (alone or in combination with other molecular targets) have been proposed for novel therapeutic uses in neuroprotection, cognitive impairment, Parkinson's disease, pain treatment, malignant carcinoid syndrome, and prostate cancer. This Perspective compares existing data on expression and signaling activity of the 5-HT(1A) receptor to a ligand with an intrinsic agonist or antagonist profile. Our purpose is also to make a complete overview, useful for underlining the features needed to select a specific pharmacological profile rather than another one. This aspect could be really interesting to consider and justify the 5-HT(1A) receptor as a new attractive target for drug discovery.
authors.affiliation: Dipartimento di Farmacia, Università degli Studi di Napoli "Federico II" , Via D. Montesano, 49, 80131, Napoli, Italy.
authors.forename: Ferdinando
authors.initials: F
authors.lastname: Fiorino
authors.forename: Beatrice
authors.initials: B
authors.lastname: Severino
authors.forename: Elisa
authors.initials: E
authors.lastname: Magli
authors.forename: Antonio
authors.initials: A
authors.lastname: Ciano
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Caliendo
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Santagada
authors.forename: Francesco
authors.initials: F
authors.lastname: Frecentese
authors.forename: Elisa
authors.initials: E
authors.lastname: Perissutti
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001921:Brain / Q000378:metabolism; D002319:Cardiovascular System / Q000187:drug effects; D002491:Central Nervous System Agents / Q000737:chemistry* / Q000494:pharmacology; D055808:Drug Discovery; D006801:Humans; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D044282:Receptor, Serotonin, 5-HT1A / Q000235:genetics / Q000502:physiology*; D058825:Serotonin 5-HT1 Receptor Agonists / Q000737:chemistry / Q000494:pharmacology; D058829:Serotonin 5-HT1 Receptor Antagonists / Q000737:chemistry / Q000494:pharmacology; D014566:Urogenital System / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D002491:Central Nervous System Agents; D010879:Piperazines; D058825:Serotonin 5-HT1 Receptor Agonists; D058829:Serotonin 5-HT1 Receptor Antagonists; D044282:Receptor, Serotonin, 5-HT1A