International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function

Nicholas M Barnes; Gerard P Ahern; Carine Becamel; Joël Bockaert; Michael Camilleri; Severine Chaumont-Dubel; Sylvie Claeysen; Kathryn A Cunningham; Kevin C Fone; Michael Gershon; Giuseppe Di Giovanni; Nathalie M Goodfellow; Adam L Halberstadt; Rachel M Hartley; Ghérici Hassaine; Katharine Herrick-Davis; Ruud Hovius; Enza Lacivita; Evelyn K Lambe; Marcello Leopoldo; Finn Olav Levy; Sarah C R Lummis; Philippe Marin; Luc Maroteaux; Andrew C McCreary; David L Nelson; John F Neumaier; Adrian Newman-Tancredi; Hugues Nury; Alexander Roberts; Bryan L Roth; Anne Roumier; Gareth J Sanger; Milt Teitler; Trevor Sharp; Carlos M Villalón; Horst Vogel; Stephanie W Watts; Daniel Hoyer

doi:10.1124/pr.118.015552

International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function

Pharmacol Rev. 2021 Jan;73(1):310-520. doi: 10.1124/pr.118.015552.

Authors

Nicholas M Barnes¹, Gerard P Ahern², Carine Becamel², Joël Bockaert², Michael Camilleri², Severine Chaumont-Dubel², Sylvie Claeysen², Kathryn A Cunningham², Kevin C Fone², Michael Gershon², Giuseppe Di Giovanni², Nathalie M Goodfellow², Adam L Halberstadt², Rachel M Hartley², Ghérici Hassaine², Katharine Herrick-Davis², Ruud Hovius², Enza Lacivita², Evelyn K Lambe², Marcello Leopoldo², Finn Olav Levy², Sarah C R Lummis², Philippe Marin², Luc Maroteaux², Andrew C McCreary², David L Nelson², John F Neumaier², Adrian Newman-Tancredi², Hugues Nury², Alexander Roberts², Bryan L Roth², Anne Roumier², Gareth J Sanger², Milt Teitler², Trevor Sharp², Carlos M Villalón², Horst Vogel², Stephanie W Watts², Daniel Hoyer²

Affiliations

¹ Neuropharmacology Research Group, College of Medical and Dental Sciences, University of Birmingham, Birmingham, United Kingdom (N.M.B., A.R.); Department of Pharmacology and Therapeutics, School of Biomedical Sciences, Faculty of Medicine, Dentistry and Health Sciences, The University of Melbourne, Parkville, Victoria, Australia (N.M.B., D.H.); Department of Pharmacology, Georgetown University Medical Center, Washington, DC (G.P.A.); Institut de Génomique Functionnelle, Université Montpellier, Centre National de la Recherche Scientifique, Institut National de la Santé et de la Recherche Médicale, Montpellier, France (C.B., J.B., S.C.-D., S.C., P.M.); Université de Montpellier, Montpellier, France (C.B., J.B., S.C.-D., S.C., P.M.); C.E.N.T.E.R. Division of Gastroenterology and Hepatology Mayo Clinic, Rochester, Minnesota (M.C.); Center for Addiction Research and Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas (K.A.C., R.M.H.); School of Life Sciences, Medical School, Queen's Medical Centre, The University of Nottingham, Nottingham, United Kingdom (K.C.F.); Department of Pathology and Cell Biology, Columbia University College of Physicians and Surgeons, New York, New York (M.G.); Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta (G.D.G.); Department of Physiology, Department of Obstetrics and Gynaecology, Department of Psychiatry, University of Toronto, Toronto, Ontario, Canada (N.M.G., E.K.L.); Department of Psychiatry, University of California San Diego, La Jolla, California (A.L.H.); Theranyx, Marseille, France (G.H.); Department of Neuroscience and Experimental Therapeutics, Albany Medical College, Albany, New York (K.H.-D.); Ecole Polytechnique Fédérale de Lausanne, Institute of Chemical Sciences and Engineering, Lausanne, Switzerland (R.H., H.V.); Department of Pharmacy-Drug Science, University of Bari Aldo Moro, Bari, Italy (E.L., M.L.); Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway (F.O.L.); Department of Biochemistry, University of Cambridge, Cambridge, United Kingdom (S.C.R.L.); INSERM UMR-S 1270, Paris, France (L.M., A.R.); Sorbonne Université, Paris, France (L.M., A.R.); Institut du Fer à Moulin, Paris, France (L.M., A.R.); Drug Development, Grunenthal GmbH, Aachen, Germany (A.C.M.); Tucson, Arizona (D.L.N.); Departments of Psychiatry and Behavioral Sciences and Pharmacology, University of Washington, Seattle, Washington (J.F.N.); Neurolixis Inc., Dana Point, California (A.N.-T.); Université Grenoble Alpes, Institut de Biologie Structurale, Grenoble, France (H.N.); CNRS, Institut de Biologie Structurale, Grenoble, France (H.N.); Commissariat à l'Energie Atomique et aux Energies Alternatives, DSV, Institut de Biologie Structurale, Grenoble, France (H.N.); Department of Pharmacology, University of North Carolina, Chapel Hill, North Carolina (B.L.R.); Blizard Institute, Barts and the London School of Medicine and Dentistry, Queen Mary University of London, London, United Kingdom (G.J.S.); Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York (M.T.); Department of Pharmacology, University of Oxford, Oxford, United Kingdom (T.S.); Cinvestav-Coapa, Pharmacobiology, Mexico City, Tlalpan, Mexico (C.M.V.); Department of Pharmacology and Toxicology, Michigan State University, East Lansing, Michigan (S.W.W.); The Florey Institute of Neuroscience and Mental Health, The University of Melbourne, Parkville, Victoria, Australia (D.H.); and Department of Molecular Medicine, The Scripps Research Institute, La Jolla, California (D.H.) n.m.barnes@bham.ac.uk d.hoyer@unimelb.edu.au.
² Neuropharmacology Research Group, College of Medical and Dental Sciences, University of Birmingham, Birmingham, United Kingdom (N.M.B., A.R.); Department of Pharmacology and Therapeutics, School of Biomedical Sciences, Faculty of Medicine, Dentistry and Health Sciences, The University of Melbourne, Parkville, Victoria, Australia (N.M.B., D.H.); Department of Pharmacology, Georgetown University Medical Center, Washington, DC (G.P.A.); Institut de Génomique Functionnelle, Université Montpellier, Centre National de la Recherche Scientifique, Institut National de la Santé et de la Recherche Médicale, Montpellier, France (C.B., J.B., S.C.-D., S.C., P.M.); Université de Montpellier, Montpellier, France (C.B., J.B., S.C.-D., S.C., P.M.); C.E.N.T.E.R. Division of Gastroenterology and Hepatology Mayo Clinic, Rochester, Minnesota (M.C.); Center for Addiction Research and Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas (K.A.C., R.M.H.); School of Life Sciences, Medical School, Queen's Medical Centre, The University of Nottingham, Nottingham, United Kingdom (K.C.F.); Department of Pathology and Cell Biology, Columbia University College of Physicians and Surgeons, New York, New York (M.G.); Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta (G.D.G.); Department of Physiology, Department of Obstetrics and Gynaecology, Department of Psychiatry, University of Toronto, Toronto, Ontario, Canada (N.M.G., E.K.L.); Department of Psychiatry, University of California San Diego, La Jolla, California (A.L.H.); Theranyx, Marseille, France (G.H.); Department of Neuroscience and Experimental Therapeutics, Albany Medical College, Albany, New York (K.H.-D.); Ecole Polytechnique Fédérale de Lausanne, Institute of Chemical Sciences and Engineering, Lausanne, Switzerland (R.H., H.V.); Department of Pharmacy-Drug Science, University of Bari Aldo Moro, Bari, Italy (E.L., M.L.); Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway (F.O.L.); Department of Biochemistry, University of Cambridge, Cambridge, United Kingdom (S.C.R.L.); INSERM UMR-S 1270, Paris, France (L.M., A.R.); Sorbonne Université, Paris, France (L.M., A.R.); Institut du Fer à Moulin, Paris, France (L.M., A.R.); Drug Development, Grunenthal GmbH, Aachen, Germany (A.C.M.); Tucson, Arizona (D.L.N.); Departments of Psychiatry and Behavioral Sciences and Pharmacology, University of Washington, Seattle, Washington (J.F.N.); Neurolixis Inc., Dana Point, California (A.N.-T.); Université Grenoble Alpes, Institut de Biologie Structurale, Grenoble, France (H.N.); CNRS, Institut de Biologie Structurale, Grenoble, France (H.N.); Commissariat à l'Energie Atomique et aux Energies Alternatives, DSV, Institut de Biologie Structurale, Grenoble, France (H.N.); Department of Pharmacology, University of North Carolina, Chapel Hill, North Carolina (B.L.R.); Blizard Institute, Barts and the London School of Medicine and Dentistry, Queen Mary University of London, London, United Kingdom (G.J.S.); Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York (M.T.); Department of Pharmacology, University of Oxford, Oxford, United Kingdom (T.S.); Cinvestav-Coapa, Pharmacobiology, Mexico City, Tlalpan, Mexico (C.M.V.); Department of Pharmacology and Toxicology, Michigan State University, East Lansing, Michigan (S.W.W.); The Florey Institute of Neuroscience and Mental Health, The University of Melbourne, Parkville, Victoria, Australia (D.H.); and Department of Molecular Medicine, The Scripps Research Institute, La Jolla, California (D.H.).

Abstract

5-HT receptors expressed throughout the human body are targets for established therapeutics and various drugs in development. Their diversity of structure and function reflects the important role 5-HT receptors play in physiologic and pathophysiological processes. The present review offers a framework for the official receptor nomenclature and a detailed understanding of each of the 14 5-HT receptor subtypes, their roles in the systems of the body, and, where appropriate, the (potential) utility of therapeutics targeting these receptors. SIGNIFICANCE STATEMENT: This review provides a comprehensive account of the classification and function of 5-hydroxytryptamine receptors, including how they are targeted for therapeutic benefit.

Publication types

Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Review

MeSH terms

Humans
Ligands
Pharmacology, Clinical*
Receptors, Serotonin
Serotonin*

Substances

Ligands
Receptors, Serotonin
Serotonin

Abstract

Publication types

MeSH terms

Substances

Grants and funding