The concise guide to PHARMACOLOGY 2025/26 : G protein‐coupled receptors

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Alexander, Stephen P. H. and Davenport, Anthony P. and Kelly, Eamonn and Gibb, Alasdair J. and Mathie, Alistair A. and Peach, Chloe J. and Veale, Emma L. and Armstrong, Jane F. and Faccenda, Elena and Harding, Simon D. and Southan, Christopher and Davies, Jamie A. and Abbracchio, Maria Pia and Abraham, George R. and Agoulnik, Alexander and Alexander, Wayne and Al‐hosaini, Khaled and Bäck, Magnus and Baker, Jillian G. and Barnes, Nicholas M. and Bathgate, Ross and Beaulieu, Jean‐Martin and Beck‐Sickinger, Annette G. and Behrens, Maik and Bennett, Kirstie A. and Bernstein, Kenneth E. and Bettler, Bernhard and Birdsall, Nigel J. M. and Blaho, Victoria A. and Bonaventure, Pascal and Boulay, Francois and Bousquet, Corinne and Bräuner‐Osborne, Hans and Brown, Andrew J. and Burnstock, Geoffrey and Busnelli, Marta and Caló, Girolamo and Caruso, Vanni and Castaño, Justo P. and Catt, Kevin J. and Ceruti, Stefania and Chazot, Paul and Chiang, Nan and Chini, Bice and Christopoulos, Arthur and Chun, Jerold and Cianciulli, Antonia and Civelli, Olivier and Clapp, Lucie H. and Couture, Réjean and Cox, Helen M. and Csaba, Zsolt and Dahlgren, Claes and Dautzenberg, Frank M. and Dent, Gordon and Douglas, Steven D. and Dournaud, Pascal and Dubocovich, Margarita L. and Eguchi, Satoru and Escher, Emanuel and Filardo, Edward J. and Fong, Tung and Forsman, Huamei Fu and Fumagalli, Marta and Gainetdinov, Raul R. and Garelja, Michael L. and de Gasparo, Marc and Gbahou, Florence and Gerard, Craig and Gershengorn, Marvin and Glass, Michelle and Gloriam, David E. and Gobeil, Fernand and Goodfriend, Theodore L. and Goudet, Cyril and Grätz, Lukas and Gregory, Karen J. and Gruber, Christian and Gundlach, Andrew L. and Hamann, Jörg and Hanson, Julien and Hartman, Deborah S. and Hauger, Richard L. and Hay, Debbie L. and Heinemann, Akos and Heitman, Laura and Herr, Deron R. and Hollenberg, Morley D. and Holliday, Nicholas D. and Holst, Birgitte and Horiuchi, Mastgugu and Hoyer, Daniel and Hunyady, László and Husain, Ahsan and IJzerman, Adriaan P. and Inagami, Tadashi and Insel, Paul A. and Jacobson, Kenneth A. and Jacobson, Laura H. and Jensen, Robert T. and Jockers, Ralf and Jonnalagadda, Deepa and Karnik, Sadashiva and Kaupmann, Klemens and Kemp, Jacqueline and Kennedy, Charles and Kihara, Yasuyuki and Kinsolving, Julia and Kitazawa, Takio and Kozielewicz, Pawel and Kreienkamp, Hans‐Jürgen and Kukkonen, Jyrki P. and Laishram, Luxmichan and Langenhan, Tobias and Langmead, Christopher J. and Larhammar, Dan and Leach, Katie and Lecca, Davide and Lee, John D. and Leeman, Susan E. and Leprince, Jérôme and Leurs, Rob and Li, Xaria X. and Liebscher, Ines and Lolait, Stephen J. and Lupp, Amelie and Macrae, Robyn and Maguire, Janet J. and Malfacini, Davide and Manning, Maurice and Marangon, Davide and Martemyanov, Kirill and Mazella, Jean and McArdle, Craig A. and Melmed, Shlomo and Michel, Martin C. and Miller, Laurence J. and Mitolo, Vincenzo and Mouillac, Bernard and Müller, Christa E. and Murphy, Philip M. and Nahon, Jean‐Louis and Neubig, Richard R. and Ngo, Tony and Norel, Xavier and Nyimanu, Duuamene and O’Carroll, Anne‐Marie and Offermanns, Stefan and Panaro, Maria Antonietta and Parmentier, Marc and Perry‐Hauser, Nicole and Pertwee, Roger G. and Pin, Jean‐Philippe and Prossnitz, Eric R. and Qin, Helena Chengxue and Quinn, Mark and Raffaele, Stefano and Ramachandran, Rithwik and Ray, Manisha and Reinscheid, Rainer K. and Buzón, Alejandro Romeral and Rondard, Philippe and Rosenkilde, Mette M. and Rovati, G. Enrico and Ruzza, Chiara and Sanger, Gareth J. and Scholz, Nicole and Schöneberg, Torsten and Schulte, Gunnar and Schulz, Stefan and Segaloff, Deborah L. and Serhan, Charles N. and Shukla, Arun K. and Singh, Khuraijam Dhanachandra and Smith, Craig M. and Smith, Nicola J. and Stäubert, Claudia and Stoddart, Leigh A. and Sugimoto, Yukihiko and Summers, Roger and Tan, Valerie P. and Thal, David M. and Thomas, Walter ( Wally) and Timmermans, Pieter B. M. W. M. and Tirupula, Kalyan and Toll, Lawrence and Tulipano, Giovanni and Unal, Hamiyet and Unger, Thomas and Valant, Celine and Vanderheyden, Patrick and Vaudry, David and Vaudry, Hubert and Verbalis, Joseph G. and Vilardaga, Jean‐Pierre and Walker, Christopher S. and Wang, Ji Ming and Ward, Donald T. and Wester, Hans‐Jürgen and Willars, Gary B. and Williams, Tom Lloyd and Woodruff, Trent M. and Wu, Huixian and Yang, Cheng and Yao, Chengcan and Ye, Richard D. and Zaidman, Nathan (2025) The concise guide to PHARMACOLOGY 2025/26 : G protein‐coupled receptors. British Journal of Pharmacology, 182 (S1). S24-S151. ISSN 1476-5381 (https://doi.org/10.1111/bph.70230)

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Abstract

The Concise Guide to Pharmacology 2025/26 marks the seventh edition in this series of biennial publications in the British Journal of Pharmacology. Presented in landscape format, the guide provides a comparative overview of the pharmacology of drug target families. The concise nature of the Concise Guide refers to the style of presentation, being clear, accessible, and well‐structured, rather than the scope of the content, which spans approximately 500 pages. The Concise Guide summarises the key pharmacological properties of around 1900 human drug targets, and nearly 7000 interactions, involving around 4400 ligands. While the content is a substantially condensed version of the more detailed information and links available at the www.guidetopharmacology.org website, the printed guide serves as a permanent, citable, point‐in‐time record, that remains stable despite ongoing updates to the online database. The full contents of this publication can be found at https://bpspubs.onlinelibrary.wiley.com/doi/10.1111/bph.70230. The Concise Guides provide expert‐curated recommendations of ‘Gold Standard’ selective pharmacological tools, available either commercially or as donations, which enable the identification of individual drug targets or families of drug targets. While the Concise Guide offers a more streamlined overview, more comprehensive information, including detailed pharmacological profiles and links to multiple online databases, is available through the Guide to Pharmacology website. The 2025/26 edition of the Concise Guide is based on material current as of mid‐2025, and supersedes all previous editions, including the 2023/24 Guide, and earlier 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), and as such provides official IUPHAR classification and nomenclature for human drug targets, where applicable. 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. Each section includes nomenclature guidance, concise summaries, information of the best available pharmacological tools, key references, and suggestions for further reading.

ORCID iDs

Alexander, Stephen P. H., Davenport, Anthony P., Kelly, Eamonn, Gibb, Alasdair J., Mathie, Alistair A., Peach, Chloe J., Veale, Emma L., Armstrong, Jane F., Faccenda, Elena, Harding, Simon D., Southan, Christopher, Davies, Jamie A., Abbracchio, Maria Pia, Abraham, George R., Agoulnik, Alexander, Alexander, Wayne, Al‐hosaini, Khaled, Bäck, Magnus, Baker, Jillian G., Barnes, Nicholas M., Bathgate, Ross, Beaulieu, Jean‐Martin, Beck‐Sickinger, Annette G., Behrens, Maik, Bennett, Kirstie A., Bernstein, Kenneth E., Bettler, Bernhard, Birdsall, Nigel J. M., Blaho, Victoria A., Bonaventure, Pascal, Boulay, Francois, Bousquet, Corinne, Bräuner‐Osborne, Hans, Brown, Andrew J., Burnstock, Geoffrey, Busnelli, Marta, Caló, Girolamo, Caruso, Vanni, Castaño, Justo P., Catt, Kevin J., Ceruti, Stefania, Chazot, Paul, Chiang, Nan, Chini, Bice, Christopoulos, Arthur, Chun, Jerold, Cianciulli, Antonia, Civelli, Olivier, Clapp, Lucie H., Couture, Réjean, Cox, Helen M., Csaba, Zsolt, Dahlgren, Claes, Dautzenberg, Frank M., Dent, Gordon, Douglas, Steven D., Dournaud, Pascal, Dubocovich, Margarita L., Eguchi, Satoru, Escher, Emanuel, Filardo, Edward J., Fong, Tung, Forsman, Huamei Fu, Fumagalli, Marta, Gainetdinov, Raul R., Garelja, Michael L., de Gasparo, Marc, Gbahou, Florence, Gerard, Craig, Gershengorn, Marvin, Glass, Michelle, Gloriam, David E., Gobeil, Fernand, Goodfriend, Theodore L., Goudet, Cyril, Grätz, Lukas, Gregory, Karen J., Gruber, Christian, Gundlach, Andrew L., Hamann, Jörg, Hanson, Julien, Hartman, Deborah S., Hauger, Richard L., Hay, Debbie L., Heinemann, Akos, Heitman, Laura, Herr, Deron R., Hollenberg, Morley D., Holliday, Nicholas D., Holst, Birgitte, Horiuchi, Mastgugu, Hoyer, Daniel, Hunyady, László, Husain, Ahsan, IJzerman, Adriaan P., Inagami, Tadashi, Insel, Paul A., Jacobson, Kenneth A., Jacobson, Laura H., Jensen, Robert T., Jockers, Ralf, Jonnalagadda, Deepa, Karnik, Sadashiva, Kaupmann, Klemens, Kemp, Jacqueline, Kennedy, Charles ORCID logoORCID: https://orcid.org/0000-0001-9661-5437, Kihara, Yasuyuki, Kinsolving, Julia, Kitazawa, Takio, Kozielewicz, Pawel, Kreienkamp, Hans‐Jürgen, Kukkonen, Jyrki P., Laishram, Luxmichan, Langenhan, Tobias, Langmead, Christopher J., Larhammar, Dan, Leach, Katie, Lecca, Davide, Lee, John D., Leeman, Susan E., Leprince, Jérôme, Leurs, Rob, Li, Xaria X., Liebscher, Ines, Lolait, Stephen J., Lupp, Amelie, Macrae, Robyn, Maguire, Janet J., Malfacini, Davide, Manning, Maurice, Marangon, Davide, Martemyanov, Kirill, Mazella, Jean, McArdle, Craig A., Melmed, Shlomo, Michel, Martin C., Miller, Laurence J., Mitolo, Vincenzo, Mouillac, Bernard, Müller, Christa E., Murphy, Philip M., Nahon, Jean‐Louis, Neubig, Richard R., Ngo, Tony, Norel, Xavier, Nyimanu, Duuamene, O’Carroll, Anne‐Marie, Offermanns, Stefan, Panaro, Maria Antonietta, Parmentier, Marc, Perry‐Hauser, Nicole, Pertwee, Roger G., Pin, Jean‐Philippe, Prossnitz, Eric R., Qin, Helena Chengxue, Quinn, Mark, Raffaele, Stefano, Ramachandran, Rithwik, Ray, Manisha, Reinscheid, Rainer K., Buzón, Alejandro Romeral, Rondard, Philippe, Rosenkilde, Mette M., Rovati, G. Enrico, Ruzza, Chiara, Sanger, Gareth J., Scholz, Nicole, Schöneberg, Torsten, Schulte, Gunnar, Schulz, Stefan, Segaloff, Deborah L., Serhan, Charles N., Shukla, Arun K., Singh, Khuraijam Dhanachandra, Smith, Craig M., Smith, Nicola J., Stäubert, Claudia, Stoddart, Leigh A., Sugimoto, Yukihiko, Summers, Roger, Tan, Valerie P., Thal, David M., Thomas, Walter ( Wally), Timmermans, Pieter B. M. W. M., Tirupula, Kalyan, Toll, Lawrence, Tulipano, Giovanni, Unal, Hamiyet, Unger, Thomas, Valant, Celine, Vanderheyden, Patrick, Vaudry, David, Vaudry, Hubert, Verbalis, Joseph G., Vilardaga, Jean‐Pierre, Walker, Christopher S., Wang, Ji Ming, Ward, Donald T., Wester, Hans‐Jürgen, Willars, Gary B., Williams, Tom Lloyd, Woodruff, Trent M., Wu, Huixian, Yang, Cheng, Yao, Chengcan, Ye, Richard D. and Zaidman, Nathan;
CORE (COnnecting REpositories)