5-HT receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on 5-HT receptors [65] and subsequently revised [59]) are, with the exception of the ionotropic 5-HT₃ class, GPCRs where the endogenous agonist is 5-hydroxytryptamine. The diversity of metabotropic 5-HT receptors is increased by alternative splicing that produces isoforms of the 5-HT_2A (non-functional), 5-HT_2C (non-functional), 5-HT₄, 5-HT₆ (non-functional) and 5-HT₇ receptors. Unique amongst the GPCRs, RNA editing produces 5-HT_2C receptor isoforms that differ in function, such as efficiency and specificity of coupling to G_q/11 and also pharmacology [14,159]. Most 5-HT receptors (except 5-ht_1e and 5-ht_5b) play specific roles mediating functional responses in different tissues (reviewed by [125,150]).

Tabulated pK_i and K_D values refer to binding to human 5-HT receptors unless indicated otherwise. The nomenclature of 5-HT_1B/5-HT_1D receptors has been revised [59]. Only the non-rodent form of the receptor was previously called 5-HT_1D: the human 5-HT_1B receptor (tabulated) displays a different pharmacology to the rodent forms of the receptor due to Thr335 of the human sequence being replaced by Asn in rodent receptors [57]. Wang et al. (2013) report X-ray structures which reveal the binding modality of ergotamine and dihydroergotamine (DHE) to the 5-HT_1B receptor in comparison with the structure of the 5-HT_2B receptor [156]; some of these drugs adopt rather different conformations depending on the target receptor [123]. Various 5-HT receptors have multiple partners in addition to G proteins, which may affect function and pharmacology [95]. NAS181 is a selective antagonist of the rodent 5-HT_1B receptor. Fananserin (LSD) and ketanserin bind with high affinity to dopamine D4 and histamine H₁ receptors respectively, and ketanserin is a potent α1 adrenoceptor antagonist, in addition to blocking 5-HT_2A receptors. Lysergic acid (LSD) and ergotamine show a strong preference for arrestin recruitment over G protein coupling at the 5-HT_2B receptor, with no such preference evident at 5-HT_1B receptors, and they also antagonise 5-HT_7A receptors [151]. DHE (dihydroergocryptine), pergolide and cabergoline also show significant preference for arrestin recruitment over G protein coupling at 5-HT_2B receptors [151]. The 5-HT_2B (and other 5-HT) receptors interact with immunocompetent cells [118]. The serotonin antagonist mesulergine was key to the discovery of the 5-HT_2C receptor [122], initially known as 5-HT_1C [4]. The human 5-HT_5A receptor may couple to several signal transduction pathways when stably expressed in C6 glioma cells [116] and rodent prefrontal cortex (layer V pyramidal neurons) [51]. The human orthologue of the mouse 5-ht_5b receptor is non-functional (stop codons); the 5-ht_1e receptor has not been cloned from mouse, or rat, impeding definition of its function [57]. In addition to accepted receptors, an 'orphan' receptor, unofficially termed 5-HT_1P, has been described [47].

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Subcommittee members: Nicholas M. Barnes (Chairperson) Neuropharmacology Research Group College of Medical and Dental Sciences University of Birmingham Edgbaston Birmingham B15 2TT UK Daniel Hoyer (Co-chairperson) Department of Pharmacology and Therapeutics School of Biomedical Sciences Faculty of Medicine, Dentistry and Health Sciences The University of Melbourne Parkville Victoria 3010 Australia Rodrigo Andrade Department of Pharmacology Wayne State University School of Medicine 540 East Canfield Detroit MI 48201 USA Joel Bockaert LaboratoDepartment of Pharmacology Wayne State University School of Medicine 540 East Canfield Detroit MI 48201 USA Amy Butler Cellular and Molecular Neuropharmacology Research Group Clinical and Experimental Medicine The Medical School, University of Birmingham Birmingham B15 2TT UK Michel Hamon UMR-677 INSERM/UPMC Faculté de Médecine Pierre et Marie Curie Site Pitié-Salpêtrière 91 Boulevard de l’hôpital 75634 Paris Cedex 13 France Julie Hensler Department of Pharmacology University of Texas Health Science Center 7703 Floyd Curl Drive San Antonia Texas 78229-3900 USA Katharine Herrick-Davis Department of Pharmacology and Neuroscience A-136, Albany Medical College Center for Neuropharmacology and Neuroscience Albany NY 12208 USA Luc Maroteaux Developmental Neurobiology Hôpital Salpêtrière 47 Blvd de l'Hôpital Paris 75651 France Graeme R. Martin Discovery-Insight 37 Erin Lane Half Moon Bay CA 94019-1770 USA John Neumaier (Past chairperson) Department of Psychiatry and Behavioral Sciences Harborview Medical Center University of Washington Seattle WA 98104 USA John A. Peters Room CB 08 Carnelley Building School of Life Sciences The University of Dundee Dundee DD1 5EH Scotland UK Bryan Roth Department of Pharmacology School of Medicine University of North Carolina Chapel Hill NC 27599 USA Trevor Sharp University Department of Pharmacology Oxford University Mansfield Road Oxford OX1 3QT UK Carlos M. Villalon Seccion de Terapeutica Experimental Departmento de Farmacologia y Toxicologia CINVESTAV IPN Adpo Postal 22026 Mexico DF 14000 Mexico

Other contributors: Gordon Baxter Pharmagene Laboratories 2A Orchard Road Royston SG8 5HD UK Theresa Branchek Synaptic Pharmaceutical Corporation 215 College Road Paramus NJ 07652-1410 USA Marlene L. Cohen Cardiovascular Pharmacology 0821 Lilly Research Laboratories MC304 Indianapolis IN 46285-0001 USA Aline Dumuis Directeur de Recherche CNRS Institut de Génomique Fonctionnelle - Dépt. de Neurobiologie UMR 5203 CNRS - U 661 INSERM - Univ. Montpellier I & II 141, rue de la Cardonille Montpellier 34094 France Richard M. Eglen PerkinElmer William Street Wellesley Hills MA 02481 USA Manfred Göthert Institut für Pharmakologie und Toxikologie Universität Bonn Reuterstrasse 2b Bonn 5300 Germany Mark Hamblin Department of Psychiatry and Behavioural Sciences Geriatric Research Education and Clinical Center (182B) Seattle Veterans Affairs Medical Center 1660 South Columbian Way Seattle WA 98108 USA Paul R. Hartig DuPont-Merck Pharmaceutical Company Experimental Station PO Box 80400 Wilmington DE 19880-0400 USA René Hen Columbia University College of Physicians and Surgeons Center for Neurobiology and Behavior 722 West 168th Street New York NY 10032 USA Rebecca Hills (Past curator) Patrick P. A. Humphrey Glaxo Institute of Applied Pharmacology Department of Pharmacology University of Cambridge Tennis Court Road Cambridge CB2 1QJ UK Klaus Peter Latté axxonis Pharma AG Schöneberger Strasse 15 (2.OG) Berlin D-10963 Germany Derek N. Middlemiss Psychiatry Research Department Smith-Kline-Beecham Pharmaceuticals New Frontiers Science Park Third Avenue Harlow CM19 5AD UK Ewan Mylecharane Department of Pharmacology University of Sydney Sydney NSW 2006 Australia Stephen J. Peroutka 1025 Tournament Drive Hillsborough CA 94010 USA Pramod R. Saxena Department of Pharmacology Erasmus Universiteit Rotterdam Postbus 1738 Rotterdam 3000 DR The Netherlands Andrew Sleight Department of Neuropharmacology Hoffman-La Roche Postfach 4002 Basel CH-4050 Switzerland Frank Yocca Preclinical CNS Research Bristol-Myers Squibb PO Box 5100 5 Research Park Wallingford CT 06492-7660 USA