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The Concise Guide to PHARMACOLOGY 2025/26: G protein‐coupled receptors
British Journal of Pharmacology, Volume 182, Issue S1, Page S24-S151, December 2025.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,Stephen P. H. Alexander, Anthony P. Davenport, Eamonn Kelly, Alasdair J. Gibb, Alistair A. Mathie, Chloe J. Peach, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Christopher Southan, Jamie A. Davies, Maria Pia Abbracchio, George R. Abraham, Alexander Agoulnik, Wayne Alexander, Khaled Al‐hosaini, Magnus Bäck, Jillian G. Baker, Nicholas M. Barnes, Ross Bathgate, Jean‐Martin Beaulieu, Annette G. Beck‐Sickinger, Maik Behrens, Kirstie A. Bennett, Kenneth E. Bernstein, Bernhard Bettler, Nigel J. M. Birdsall, Victoria A. Blaho, Pascal Bonaventure, Francois Boulay, Corinne Bousquet, Hans Bräuner‐Osborne, Andrew J. Brown, Geoffrey Burnstock, Marta Busnelli, Girolamo Caló, Vanni Caruso, Justo P. Castaño, Kevin J. Catt, Stefania Ceruti, Paul Chazot, Nan Chiang, Bice Chini, Arthur Christopoulos, Jerold Chun, Antonia Cianciulli, Olivier Civelli, Lucie H. Clapp, Réjean Couture, Helen M. Cox, Zsolt Csaba, Claes Dahlgren, Frank M. Dautzenberg, Gordon Dent, Steven D. Douglas, Pascal Dournaud, Margarita L. Dubocovich, Satoru Eguchi, Emanuel Escher, Edward J. Filardo, Tung Fong, Huamei Fu Forsman, Marta Fumagalli, Raul R. Gainetdinov, Michael L. Garelja, Marc de Gasparo, Florence Gbahou, Craig Gerard, Marvin Gershengorn, Michelle Glass, David E. Gloriam, Fernand Gobeil, Theodore L. Goodfriend, Cyril Goudet, Lukas Grätz, Karen J. Gregory, Christian Gruber, Andrew L. Gundlach, Jörg Hamann, Julien Hanson, Deborah S. Hartman, Richard L. Hauger, Debbie L. Hay, Akos Heinemann, Laura Heitman, Deron R. Herr, Morley D. Hollenberg, Nicholas D. Holliday, Birgitte Holst, Mastgugu Horiuchi, Daniel Hoyer, László Hunyady, Ahsan Husain, Adriaan P. IJzerman, Tadashi Inagami, Paul A. Insel, Kenneth A. Jacobson, Laura H. Jacobson, Robert T. Jensen, Ralf Jockers, Deepa Jonnalagadda, Sadashiva Karnik, Klemens Kaupmann, Jacqueline Kemp, Charles Kennedy, Yasuyuki Kihara, Julia Kinsolving, Takio Kitazawa, Pawel Kozielewicz, Hans‐Jürgen Kreienkamp, Jyrki P. Kukkonen, Luxmichan Laishram, Tobias Langenhan, Christopher J. Langmead, Dan Larhammar, Katie Leach, Davide Lecca, John D. Lee, Susan E. Leeman, Jérôme Leprince, Rob Leurs, Xaria X. Li, Ines Liebscher, Stephen J. Lolait, Amelie Lupp, Robyn Macrae, Janet J. Maguire, Davide Malfacini, Maurice Manning, Davide Marangon, Kirill Martemyanov, Jean Mazella, Craig A. McArdle, Shlomo Melmed, Martin C. Michel, Laurence J. Miller, Vincenzo Mitolo, Bernard Mouillac, Christa E. Müller, Philip M. Murphy, Jean‐Louis Nahon, Richard R. Neubig, Tony Ngo, Xavier Norel, Duuamene Nyimanu, Anne‐Marie O’Carroll, Stefan Offermanns, Maria Antonietta Panaro, Marc Parmentier, Nicole Perry‐Hauser, Roger G. Pertwee, Jean‐Philippe Pin, Eric R. Prossnitz, Helena Chengxue Qin, Mark Quinn, Stefano Raffaele, Rithwik Ramachandran, Manisha Ray, Rainer K. Reinscheid, Alejandro Romeral Buzón, Philippe Rondard, Mette M. Rosenkilde, G. Enrico Rovati, Chiara Ruzza, Gareth J. Sanger, Nicole Scholz, Torsten Schöneberg, Gunnar Schulte, Stefan Schulz, Deborah L. Segaloff, Charles N. Serhan, Arun K. Shukla, Khuraijam Dhanachandra Singh, Craig M. Smith, Nicola J. Smith, Claudia Stäubert, Leigh A. Stoddart, Yukihiko Sugimoto, Roger Summers, Valerie P. Tan, David M. Thal, Walter ( Wally) Thomas, Pieter B. M. W. M. Timmermans, Kalyan Tirupula, Lawrence Toll, Giovanni Tulipano, Hamiyet Unal, Thomas Unger, Celine Valant, Patrick Vanderheyden, David Vaudry, Hubert Vaudry, Joseph G. Verbalis, Jean‐Pierre Vilardaga, Christopher S. Walker, Ji Ming Wang, Donald T. Ward, Hans‐Jürgen Wester, Gary B. Willars, Tom Lloyd Williams, Trent M. Woodruff, Huixian Wu, Cheng Yang, Chengcan Yao, Richard D. Ye, Nathan Zaidman +206 morewiley +1 more sourceSerelaxin Elicits Bronchodilation and Enhances β-Adrenoceptor-mediated Airway Relaxation
Frontiers in Pharmacology, 2016 Treatment with β-adrenoceptor agonists does not fully overcome the symptoms associated with severe asthma. Serelaxin elicits potent uterine and vascular relaxation via its cognate receptor, RXFP1, and nitric oxide (NO) signaling, and is being clinically ...Maggie Lam, Simon G Royce, Chantal Donovan, Maria Jelinic, Laura J Parry, Chrishan S Samuel, Jane Elizabeth Bourke +6 moredoaj +1 more sourceIdentification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1 [PDF]
Nature Communications, 2013 The anti-fibrotic, vasodilatory and pro-angiogenic therapeutic properties of recombinant relaxin peptide hormone have been investigated in several diseases, and recent clinical trial data has shown benefit in treating acute heart failure. However, the remodelling capacity of these peptide hormones is difficult to study in chronic settings because of ...Jingbo, Xiao, Zaohua, Huang, Catherine Z, Chen, Irina U, Agoulnik, Noel, Southall, Xin, Hu, Raisa E, Jones, Marc, Ferrer, Wei, Zheng, Alexander I, Agoulnik, Juan J, Marugan +10 moreopenaire +2 more sourcesRelaxin‐2 Ameliorates Spinal Cord Injury by Inhibiting Microglia Activation
The Kaohsiung Journal of Medical Sciences, Volume 41, Issue 9, September 2025.ABSTRACT
This study aims to assess the therapeutic effectiveness of Relaxin‐2 (RLN‐2) in promoting functional recovery and neuroprotection following spinal cord injury (SCI) in mice. Furthermore, continuous subcutaneous infusion of Serelaxin (0.5 mg/kg/day; human recombinant relaxin‐2) improved neurological recovery, as evidenced by higher Basso ...Ji‐Huan Wang, Hong‐Biao Sheng, Jun‐Kun Li +2 morewiley +1 more sourceDistinct activation modes of the Relaxin Family Peptide Receptor 2 in response to insulin-like peptide 3 and relaxin
Scientific Reports, 2017 Relaxin family peptide receptor 2 (RXFP2) is a GPCR known for its role in reproductive function. It is structurally related to the human relaxin receptor RXFP1 and can be activated by human gene-2 (H2) relaxin as well as its cognate ligand insulin-like ...Shoni Bruell, Ashish Sethi, Nicholas Smith, Daniel J. Scott, Mohammed Akhter Hossain, Qing-Ping Wu, Zhan-Yun Guo, Emma J. Petrie, Paul R. Gooley, Ross A. D. Bathgate +9 moredoaj +1 more sourceThe extracellular matrix and insulin resistance [PDF]
, 2015 The extracellular matrix (ECM) is a highly dynamic compartment that undergoes remodeling as a result of injury and repair. Over the past decade, mounting evidence in humans and rodents suggest that ECM remodeling is associated with diet-induced insulin ...Ashley S. Williams, Bataller, Berria, Bertola, Bisht, Bisht, Bisht, Bonner, Bonner, Brew, Carmiel-Haggai, Catalan, Catalan, Chajara, Cheung, Cheung, Dasu, David H. Wasserman, Day, Delcommenne, Demeulemeester, Derosa, Dixon, Duckworth, Duckworth, El Annabi, Eng, Farrell, Field, Friedman, Friedman, Gardner, Gheyara, Gkretsi, Gressner, Groh, Gullberg, Halberg, Hanks, Harrison, Hill, Hong, Hopps, Huang, Huang, Huber, Hynes, Hynes, Ilic, Inoue, Irwin, Jansson, Jaskiewicz, Jaworski, Jiang, Kang, Kang, Kang, Keophiphath, Khan, Kodama, Kodama, Lewis, Li Kang, Madison, Maher, Martinez-Hernandez, McCuskey, Menghini, Menghini, Moser, Pasarica, Persad, Plows, Postic, Pozzi, Qian, Richardson, Sakai, Schlaepfer, Schuppan, Signorelli, Solomon, Sun, Sun, Tam, Thrailkill, Tinahones, Toole, Troussard, Varma, Vaynberg, Volpes, Wada, Wang, Wang, Watts, White, Williams, Yadav, Zamurs, Zhang, Zong +102 morecore +2 more sourcesRecent advances of nanomaterials in imaging liver fibrosis
BMEMat, Volume 3, Issue 2, June 2025.Schematic summary on the latest strategies of liver fibrosis imaging based on various nanomaterials. Abstract
Liver fibrosis is a pathological process resulting from prolonged exposure to various injury factors. It is characterized by the abnormal proliferation and activation of hepatic stellate cells and excessive deposition of extracellular matrix ...Jin Cui, Shuxuan Zhang, Xueli Xu, Ke Ren, Mengzhen Dong, Zhaokun Nie, Yang Xu, Xiaohui Dai, Peng Xu, Shuo Sun, Xinya Zhao, Xiao Sun +11 morewiley +1 more sourceRelaxin signals through a RXFP1-pERK-nNOS-NO-cGMP-dependent pathway to up-regulate matrix metalloproteinases: the additional involvement of iNOS. [PDF]
PLoS ONE, 2012 The hormone, relaxin, inhibits aberrant myofibroblast differentiation and collagen deposition by disrupting the TGF-β1/Smad2 axis, via its cognate receptor, Relaxin Family Peptide Receptor 1 (RXFP1), extracellular signal-regulated kinase (ERK)1/2 ...Bryna Suet Man Chow, Elaine Guo Yan Chew, Chongxin Zhao, Ross A D Bathgate, Tim D Hewitson, Chrishan S Samuel +5 moredoaj +1 more sourceRelaxin mimetic in pulmonary hypertension associated with left heart disease: Design and rationale of Re‐PHIRE
ESC Heart Failure, Volume 12, Issue 3, Page 1956-1964, June 2025.Abstract Aims
Despite receiving guideline‐directed medical heart failure (HF) therapy, patients with pulmonary hypertension associated with left heart disease (PH‐LHD) experience higher mortality and hospitalization rates than the general HF population.Marcin Ufnal, Kathleen Connolly, Marcus Millegard, Elena Surkova, Marco Guazzi, Diana Bonderman, Justin Ezekowitz, Finn Gustafsson, Michał Ciurzyński, Raquel López Vilella, Tariq Ahmad, Roy Gardner, Pavel Jansa, Sandra van Wijk, Koichiro Kinugawa, Erik Björklund, Zhi‐Cheng Jing, Stephan Rosenkranz +17 morewiley +1 more sourceGene co-expression analysis identifies brain regions and cell types involved in migraine pathophysiology [PDF]
, 2016 Migraine is a common disabling neurovascular brain disorder typically characterised by attacks of severe headache and associated with autonomic and neurological symptoms. Migraine is caused by an interplay of genetic and environmental factors.Boomsma, D.I. (Dorret), Chasman, D.I. (Daniel), Dermitzakis, E.T. (Emmanouil), Dimas, A.S. (Antigone), Duijn, C.M. (Cornelia) van, Eising, E., Ferrari, M.D. (Michel), Huisman, S.M.H. (Sjoerd M. H.), Ikram, M.A. (Arfan), Jarvelin, M.-R. (Marjo-Riitta), Kaprio, J. (Jaakko), Kubisch, C. (Christian), Kurth, T. (Tobias), Lelieveldt, B.P.F. (Boudewijn), Maagdenberg, A.M.J.M. (Arn), Mahfouz, A. (Ahmed), Müller-Myhsok, B. (Bertram), Palotie, A. (Aarno), Quaye, L. (Lydia), Reinders, M.J. (Marcel), Smith, A.V. (Davey), Stam, A.H. (Anine), Stefansson, K. (Kari), Strachan, D.P. (David P.), Terwindt, G.M. (Gisela), Vijfhuizen, L.S. (Lisanne S.), Winsvold, B.S. (Bendik), Zwart, J-A. (John-Anker), Zwart, J-A. (John-Anker) +28 morecore +1 more source