THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors

Stephen Ph Alexander¹, Arthur Christopoulos², Anthony P Davenport³, Eamonn Kelly⁴, Alistair Mathie⁵, John A Peters⁶, Emma L Veale⁷, Jane F Armstrong⁸, Elena Faccenda⁸, Simon D Harding⁸, Adam J Pawson⁸, Christopher Southan⁸, Jamie A Davies⁸, Maria Pia Abbracchio⁹, Wayne Alexander¹⁰, Khaled Al-Hosaini¹¹, Magnus Bäck¹², Nicholas M Barnes¹³, Ross Bathgate¹⁴, Jean-Martin Beaulieu¹⁵, Kenneth E Bernstein¹⁶, Bernhard Bettler¹⁷, Nigel J M Birdsall¹⁸, Victoria Blaho¹⁹, Francois Boulay²⁰, Corinne Bousquet²¹, Hans Bräuner-Osborne²², Geoffrey Burnstock²³, Girolamo Caló²⁴, Justo P Castaño²⁵, Kevin J Catt²⁶, Stefania Ceruti⁹, Paul Chazot²⁷, Nan Chiang²⁸, Bice Chini²⁹, Jerold Chun³⁰, Antonia Cianciulli³¹, Olivier Civelli³², Lucie H Clapp³³, Réjean Couture³⁴, Zsolt Csaba³⁵, Claes Dahlgren³⁶, Gordon Dent³⁷, Khuraijam Dhanachandra Singh³⁸, Steven D Douglas³⁹, Pascal Dournaud³⁵, Satoru Eguchi⁴⁰, Emanuel Escher⁴¹, Edward J Filardo⁴², Tung Fong⁴³, Marta Fumagalli⁹, Raul R Gainetdinov⁴⁴, Marc de Gasparo⁴⁵, Craig Gerard²⁸, Marvin Gershengorn²⁶, Fernand Gobeil⁴¹, Theodore L Goodfriend⁴⁶, Cyril Goudet⁴⁷, Karen J Gregory⁴⁸, Andrew L Gundlach¹⁴, Jörg Hamann⁴⁹, Julien Hanson⁵⁰, Richard L Hauger³⁰, Debbie L Hay⁵¹, Akos Heinemann⁵², Morley D Hollenberg⁵³, Nicholas D Holliday⁵⁴, Mastgugu Horiuchi⁵⁵, Daniel Hoyer⁵⁶, László Hunyady⁵⁷, Ahsan Husain⁵⁸, Adriaan P IJzerman⁵⁹, Tadashi Inagami⁶⁰, Kenneth A Jacobson²⁶, Robert T Jensen²⁶, Ralf Jockers³⁵, Deepa Jonnalagadda¹⁹, Sadashiva Karnik⁶¹, Klemens Kaupmann⁶², Jacqueline Kemp³⁸, Charles Kennedy⁶³, Yasuyuki Kihara¹⁹, Takio Kitazawa⁶⁴, Pawel Kozielewicz⁶⁵, Hans-Jürgen Kreienkamp⁶⁶, Jyrki P Kukkonen⁶⁷, Tobias Langenhan⁶⁸, Katie Leach⁴⁸, Davide Lecca⁹, John D Lee⁶⁹, Susan E Leeman⁷⁰, Jérôme Leprince⁷¹, Xaria X Li⁶⁹, Tom Lloyd Williams⁷², Stephen J Lolait⁷³, Amelie Lupp⁷⁴, Robyn Macrae⁷², Janet Maguire⁷², Jean Mazella⁷⁵, Craig A McArdle⁷³, Shlomo Melmed¹⁶, Martin C Michel⁷⁶, Laurence J Miller⁷⁷, Vincenzo Mitolo³¹, Bernard Mouillac⁴⁷, Christa E Müller⁷⁸, Philip Murphy⁷⁹, Jean-Louis Nahon⁷⁵, Tony Ngo¹⁹, Xavier Norel³⁵, Duuamene Nyimanu⁷², Anne-Marie O'Carroll⁷³, Stefan Offermanns⁸⁰, Maria Antonietta Panaro³¹, Marc Parmentier⁸¹, Roger G Pertwee⁸², Jean-Philippe Pin⁸³, Eric R Prossnitz⁸⁴, Mark Quinn⁸⁵, Rithwik Ramachandran⁸⁶, Manisha Ray¹⁹, Rainer K Reinscheid⁷⁴, Philippe Rondard⁸³, G Enrico Rovati⁹, Chiara Ruzza⁸⁷, Gareth J Sanger⁸⁸, Torsten Schöneberg⁸⁹, Gunnar Schulte⁶⁵, Stefan Schulz⁷⁴, Deborah L Segaloff⁴², Charles N Serhan²⁸, Leigh A Stoddart⁵⁴, Yukihiko Sugimoto⁹⁰, Roger Summers⁹¹, Valerie P Tan³⁰, David Thal⁹¹, Walter Wally Thomas⁹², Pieter B M W M Timmermans⁹³, Kalyan Tirupula³⁸, Giovanni Tulipano⁹⁴, Hamiyet Unal⁹⁵, Thomas Unger⁹⁶, Celine Valant⁹¹, Patrick Vanderheyden⁸¹, David Vaudry⁷¹, Hubert Vaudry⁷¹, Jean-Pierre Vilardaga⁹⁷, Christopher S Walker⁹⁸, Ji Ming Wang⁹⁹, Donald T Ward¹⁰⁰, Hans-Jürgen Wester¹⁰¹, Gary B Willars¹⁰², Trent M Woodruff⁶⁹, Chengcan Yao¹⁰³, Richard D Ye¹⁰⁴

Affiliations

¹ School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.
² Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria 3052, Australia.
³ Clinical Pharmacology Unit, University of Cambridge, Cambridge, CB2 0QQ, UK.
⁴ School of Physiology, Pharmacology and Neuroscience, University of Bristol, Bristol, BS8 1TD, UK.
⁵ School of Engineering, Arts, Science and Technology, University of Suffolk, Ipswich, IP4 1QJ, UK.
⁶ Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK.
⁷ Medway School of Pharmacy, The Universities of Greenwich and Kent at Medway, Anson Building, Central Avenue, Chatham Maritime, Chatham, Kent, ME4 4TB, UK.
⁸ Centre for Discovery Brain Sciences, University of Edinburgh, Edinburgh, EH8 9XD, UK.
⁹ University of Milan, Milan, Italy.
¹⁰ Emory University, Atlanta, USA.
¹¹ King Saud University, Riyadh, Kingdom of Saudi Arabia.
¹² Karolinska University Hospital, Stockholm, Sweden.
¹³ University of Birmingham, Birmingham, UK.
¹⁴ Florey Institute of Neuroscience and Mental Health, Melbourne, Australia.
¹⁵ University of Toronto, Toronto, Canada.
¹⁶ Cedars-Sinai Medical Center, Los Angeles, USA.
¹⁷ University of Basel, Basel, Switzerland.
¹⁸ The Francis Crick Institute, London, UK.
¹⁹ Sanford Burnham Prebys Medical Discovery Institute, La Jolla, USA.
²⁰ University of Grenoble Alpes, Grenoble, France.
²¹ French Institute of Health and Medical Research(INSERM), Toulouse, France.
²² University of Copenhagen, Copenhagen, Denmark.
²³ University College London, Melbourne, Australia.
²⁴ University of Padova, Padova, Italy.
²⁵ University of Córdoba, Córdoba, Spain.
²⁶ National Institute of Health, Bethesda, USA.
²⁷ Durham University, Durham, UK.
²⁸ Harvard University, Boston, MA, USA.
²⁹ University of Milan Bicocca, Vedano al Lambro, Italy.
³⁰ University of California San Diego, La Jolla, USA.
³¹ University of Bari, Bari, Italy.
³² University of California Irvine, Irvine, USA.
³³ University College London, London, UK.
³⁴ University of Montréal, Montréal, Canada.
³⁵ French Institute of Health and Medical Research(INSERM), Paris, France.
³⁶ University of Gothenburg, Gothenburg, Sweden.
³⁷ Keele University, Keele, UK.
³⁸ Cleveland Clinic Lerner Research Institute, Cleveland, USA.
³⁹ University of Pennsylvania, Pennsylvania, USA.
⁴⁰ Temple University, Philadelphia, USA.
⁴¹ University of Sherbrooke, Sherbrooke, Canada.
⁴² University of Iowa, Iowa City, USA.
⁴³ Labcorp Drug Development, Somerset, USA.
⁴⁴ Saint Petersburg State University, Saint-Petersburg, Russia.
⁴⁵ MG Consulting Co, Basel, Switzerland.
⁴⁶ University of Wisconsin, Madison, USA.
⁴⁷ French National Centre for Scientific Research, Montpellier, France.
⁴⁸ Monash University, Parkville, Australia.
⁴⁹ Amsterdam University, Amsterdam, The Netherlands.
⁵⁰ University of Liège, Liège, Belgium.
⁵¹ University of Otago, Dunedin, New Zealand.
⁵² Medical University of Graz, Graz, Austria.
⁵³ University of Calgary, Calgary, Canada.
⁵⁴ University of Nottingham, Nottingham, UK.
⁵⁵ Ehime University, Ehime, Japan.
⁵⁶ University of Melbourne, Melbourne, Australia.
⁵⁷ Semmelweis University, Budapest, Hungary.
⁵⁸ Emory University, Birmingham, USA.
⁵⁹ Leiden University, Leiden, The Netherlands.
⁶⁰ Vanderbilt University, Nashville, USA.
⁶¹ Lerner Research Institute, Cleveland, USA.
⁶² Novartis, Basel, Switzerland.
⁶³ Strathclyde University, Glasgow, UK.
⁶⁴ Rakuno Gakuen University, Ebetsu, Japan.
⁶⁵ Karolinska Institute, Stockholm, Sweden.
⁶⁶ University of Hamburg, Hamburg, Germany.
⁶⁷ University of Helsinki, Helsinki, Finland.
⁶⁸ Leipzig University, Leipzig, Germany.
⁶⁹ University of Queensland, Brisbane, Australia.
⁷⁰ Boston University, Boston, MA, USA.
⁷¹ University of Rouen, Rouen, France.
⁷² University of Cambridge, Cambridge, UK.
⁷³ University of Bristol, Bristol, UK.
⁷⁴ Friedrich Schiller University Jena, Jena, Germany.
⁷⁵ French National Centre for Scientific Research(CNRS), Valbonne, France.
⁷⁶ Johannes Gutenberg University Mainz, Mainz, Germany.
⁷⁷ Mayo Foundation for Medical Education and Research, Scottsdale, USA.
⁷⁸ University of Bonn, Bonn, Germany.
⁷⁹ Edge Hill University, Bethesda, USA.
⁸⁰ Max Planck Institute for Heart and Lung Research, Bad Nauheim, Germany.
⁸¹ Free University of Brussels, Brussels, Belgium.
⁸² University of Aberdeen, Aberdeen, UK.
⁸³ University of Montpellier, Montpellier, France.
⁸⁴ University of New Mexico, Albuquerque, USA.
⁸⁵ Montana State University, Bozeman, USA.
⁸⁶ University of Calgary, London, Canada.
⁸⁷ University of Ferrara, Ferrara, Italy.
⁸⁸ Queen Mary University of London, London, UK.
⁸⁹ University of Leipzig, Leipzig, Germany.
⁹⁰ Kumamoto University, Kumamoto, Japan.
⁹¹ Monash University, Melbourne, Australia.
⁹² University of Queensland, Queensland, Australia.
⁹³ Kosan Biosciences, Inc., San Francisco, CA, USA.
⁹⁴ University of Brescia, Brescia, Italy.
⁹⁵ Cleveland Clinic, Cleveland, USA.
⁹⁶ Maastricht University, Maastricht, The Netherlands.
⁹⁷ University of Pittsburgh, Pittsburgh, USA.
⁹⁸ University of Auckland, Auckland, New Zealand.
⁹⁹ National Institute of Health, Frederick, USA.
¹⁰⁰ University of Manchester, Manchester, UK.
¹⁰¹ Technical University of Munich, Munich, Germany.
¹⁰² University of Leicester, Leicester, UK.
¹⁰³ University of Edinburgh, Edinburgh, UK.
¹⁰⁴ University of Illinois, Chicago, USA.

PMID: 34529832
DOI: 10.1111/bph.15538

Free article

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors

Stephen Ph Alexander et al. Br J Pharmacol. 2021 Oct.

Free article

. 2021 Oct:178 Suppl 1:S27-S156.

doi: 10.1111/bph.15538.

Authors

Affiliations

¹ School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.
² Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria 3052, Australia.
³ Clinical Pharmacology Unit, University of Cambridge, Cambridge, CB2 0QQ, UK.
⁴ School of Physiology, Pharmacology and Neuroscience, University of Bristol, Bristol, BS8 1TD, UK.
⁵ School of Engineering, Arts, Science and Technology, University of Suffolk, Ipswich, IP4 1QJ, UK.
⁶ Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK.
⁷ Medway School of Pharmacy, The Universities of Greenwich and Kent at Medway, Anson Building, Central Avenue, Chatham Maritime, Chatham, Kent, ME4 4TB, UK.
⁸ Centre for Discovery Brain Sciences, University of Edinburgh, Edinburgh, EH8 9XD, UK.
⁹ University of Milan, Milan, Italy.
¹⁰ Emory University, Atlanta, USA.
¹¹ King Saud University, Riyadh, Kingdom of Saudi Arabia.
¹² Karolinska University Hospital, Stockholm, Sweden.
¹³ University of Birmingham, Birmingham, UK.
¹⁴ Florey Institute of Neuroscience and Mental Health, Melbourne, Australia.
¹⁵ University of Toronto, Toronto, Canada.
¹⁶ Cedars-Sinai Medical Center, Los Angeles, USA.
¹⁷ University of Basel, Basel, Switzerland.
¹⁸ The Francis Crick Institute, London, UK.
¹⁹ Sanford Burnham Prebys Medical Discovery Institute, La Jolla, USA.
²⁰ University of Grenoble Alpes, Grenoble, France.
²¹ French Institute of Health and Medical Research(INSERM), Toulouse, France.
²² University of Copenhagen, Copenhagen, Denmark.
²³ University College London, Melbourne, Australia.
²⁴ University of Padova, Padova, Italy.
²⁵ University of Córdoba, Córdoba, Spain.
²⁶ National Institute of Health, Bethesda, USA.
²⁷ Durham University, Durham, UK.
²⁸ Harvard University, Boston, MA, USA.
²⁹ University of Milan Bicocca, Vedano al Lambro, Italy.
³⁰ University of California San Diego, La Jolla, USA.
³¹ University of Bari, Bari, Italy.
³² University of California Irvine, Irvine, USA.
³³ University College London, London, UK.
³⁴ University of Montréal, Montréal, Canada.
³⁵ French Institute of Health and Medical Research(INSERM), Paris, France.
³⁶ University of Gothenburg, Gothenburg, Sweden.
³⁷ Keele University, Keele, UK.
³⁸ Cleveland Clinic Lerner Research Institute, Cleveland, USA.
³⁹ University of Pennsylvania, Pennsylvania, USA.
⁴⁰ Temple University, Philadelphia, USA.
⁴¹ University of Sherbrooke, Sherbrooke, Canada.
⁴² University of Iowa, Iowa City, USA.
⁴³ Labcorp Drug Development, Somerset, USA.
⁴⁴ Saint Petersburg State University, Saint-Petersburg, Russia.
⁴⁵ MG Consulting Co, Basel, Switzerland.
⁴⁶ University of Wisconsin, Madison, USA.
⁴⁷ French National Centre for Scientific Research, Montpellier, France.
⁴⁸ Monash University, Parkville, Australia.
⁴⁹ Amsterdam University, Amsterdam, The Netherlands.
⁵⁰ University of Liège, Liège, Belgium.
⁵¹ University of Otago, Dunedin, New Zealand.
⁵² Medical University of Graz, Graz, Austria.
⁵³ University of Calgary, Calgary, Canada.
⁵⁴ University of Nottingham, Nottingham, UK.
⁵⁵ Ehime University, Ehime, Japan.
⁵⁶ University of Melbourne, Melbourne, Australia.
⁵⁷ Semmelweis University, Budapest, Hungary.
⁵⁸ Emory University, Birmingham, USA.
⁵⁹ Leiden University, Leiden, The Netherlands.
⁶⁰ Vanderbilt University, Nashville, USA.
⁶¹ Lerner Research Institute, Cleveland, USA.
⁶² Novartis, Basel, Switzerland.
⁶³ Strathclyde University, Glasgow, UK.
⁶⁴ Rakuno Gakuen University, Ebetsu, Japan.
⁶⁵ Karolinska Institute, Stockholm, Sweden.
⁶⁶ University of Hamburg, Hamburg, Germany.
⁶⁷ University of Helsinki, Helsinki, Finland.
⁶⁸ Leipzig University, Leipzig, Germany.
⁶⁹ University of Queensland, Brisbane, Australia.
⁷⁰ Boston University, Boston, MA, USA.
⁷¹ University of Rouen, Rouen, France.
⁷² University of Cambridge, Cambridge, UK.
⁷³ University of Bristol, Bristol, UK.
⁷⁴ Friedrich Schiller University Jena, Jena, Germany.
⁷⁵ French National Centre for Scientific Research(CNRS), Valbonne, France.
⁷⁶ Johannes Gutenberg University Mainz, Mainz, Germany.
⁷⁷ Mayo Foundation for Medical Education and Research, Scottsdale, USA.
⁷⁸ University of Bonn, Bonn, Germany.
⁷⁹ Edge Hill University, Bethesda, USA.
⁸⁰ Max Planck Institute for Heart and Lung Research, Bad Nauheim, Germany.
⁸¹ Free University of Brussels, Brussels, Belgium.
⁸² University of Aberdeen, Aberdeen, UK.
⁸³ University of Montpellier, Montpellier, France.
⁸⁴ University of New Mexico, Albuquerque, USA.
⁸⁵ Montana State University, Bozeman, USA.
⁸⁶ University of Calgary, London, Canada.
⁸⁷ University of Ferrara, Ferrara, Italy.
⁸⁸ Queen Mary University of London, London, UK.
⁸⁹ University of Leipzig, Leipzig, Germany.
⁹⁰ Kumamoto University, Kumamoto, Japan.
⁹¹ Monash University, Melbourne, Australia.
⁹² University of Queensland, Queensland, Australia.
⁹³ Kosan Biosciences, Inc., San Francisco, CA, USA.
⁹⁴ University of Brescia, Brescia, Italy.
⁹⁵ Cleveland Clinic, Cleveland, USA.
⁹⁶ Maastricht University, Maastricht, The Netherlands.
⁹⁷ University of Pittsburgh, Pittsburgh, USA.
⁹⁸ University of Auckland, Auckland, New Zealand.
⁹⁹ National Institute of Health, Frederick, USA.
¹⁰⁰ University of Manchester, Manchester, UK.
¹⁰¹ Technical University of Munich, Munich, Germany.
¹⁰² University of Leicester, Leicester, UK.
¹⁰³ University of Edinburgh, Edinburgh, UK.
¹⁰⁴ University of Illinois, Chicago, USA.

PMID: 34529832
DOI: 10.1111/bph.15538

Abstract

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes over 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/bph.15538. G protein-coupled receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2021, and supersedes data presented in the 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

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THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors

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THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors

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