Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2

Wright, P.D., McCoull, D., Walsh, Y., Large, J.M., Hadrys, B.W., Gaurilcikaite, E., Byrom, L., Veale, E.L., Jerman, J. and Mathie, A. 2019. Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2. Biochemical and Biophysical Research Communications. 520 (1), pp. 35-40. https://doi.org/10.1016/j.bbrc.2019.09.093

TitlePranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2
TypeJournal article
AuthorsWright, P.D., McCoull, D., Walsh, Y., Large, J.M., Hadrys, B.W., Gaurilcikaite, E., Byrom, L., Veale, E.L., Jerman, J. and Mathie, A.
Abstract

TREK2 (KCNK10, K2P10.1) is a two-pore domain potassium (K2P) channel and a potential target for the treatment of pain. Like the majority of the K2P superfamily, there is currently a lack of useful pharmacological tools to study TREK2. Here we present a strategy for identifying novel TREK2 activators. A cell-based thallium flux assay was developed and used to screen a library of drug-like molecules, from which we identified the CysLT1 antagonist Pranlukast as a novel activator of TREK2. This compound was selective for TREK2 versus TREK1 and showed no activity at TRAAK. Pranlukast was also screened against other members of the K2P superfamily. Several close analogues of Pranlukast and other CysLT1 antagonists were also tested for their ability to activate K2P channels. Consistent with previous work, structure activity relationships showed that subtle structural changes to these analogues completely attenuated the activation of TREK2, whereas for TREK1, analogues moved from activators to inhibitors. Pranlukast’s activity was also confirmed using whole-cell patch clamp electrophysiology. Studies using mutant forms of TREK2 suggest Pranlukast does not bind in the K2P modulator pocket or the BL-1249 binding site. Pranlukast therefore represents a novel tool by which to study the mechanism of TREK2 activation.

JournalBiochemical and Biophysical Research Communications
Journal citation520 (1), pp. 35-40
ISSN1090-2104
Year2019
PublisherElsevier
Publisher's version
License
CC BY 4.0
File Access Level
Open (open metadata and files)
Digital Object Identifier (DOI)https://doi.org/10.1016/j.bbrc.2019.09.093
PubMed ID31564414
Publication dates
PublishedSep 2019

Related outputs

TASK-3, two-pore potassium channels, contribute to circadian rhythms in the electrical properties of the suprachiasmatic nucleus and play a role in driving stable behavioural photic entrainment.
Steponenaite, A., Lalic, T., Atkinson, L., Tanday, N., Brown, L., Mathie, A., Cader, Z.M. and Lall, G.S. 2024. TASK-3, two-pore potassium channels, contribute to circadian rhythms in the electrical properties of the suprachiasmatic nucleus and play a role in driving stable behavioural photic entrainment. Chronobiology International. 41 (6), pp. 802-816. https://doi.org/10.1080/07420528.2024.2351515

The Contribution of Genetic Sequencing Information to the Identification and Functional Characterization of Two-Pore Domain Potassium (K2P) Channels as Viable Therapeutic Targets
Alistair Mathie, Samuel R. Bourne, Rachel Forfar, Walter E. Perfect and Emma L. Veale 2024. The Contribution of Genetic Sequencing Information to the Identification and Functional Characterization of Two-Pore Domain Potassium (K2P) Channels as Viable Therapeutic Targets. in: Stephens, G. and Stevens, E. (ed.) Ion Channels as Targets in Drug Discovery Springer Nature. pp. 199-220

Screening for atrial fibrillation in care homes using pulse palpation and the AliveCor Kardia Mobile® device: a comparative cross-sectional pilot study
V. Savickas, A. J. Stewart, V. J. Short, A. Mathie, S. K. Bhamra, E. L. Veale and S. A. Corlett 2024. Screening for atrial fibrillation in care homes using pulse palpation and the AliveCor Kardia Mobile® device: a comparative cross-sectional pilot study. International Journal of Clinical Pharmacy. 46, pp. 529-535. https://doi.org/10.1007/s11096-023-01672-z

The Concise Guide to PHARMACOLOGY 2023/24: Transporters
Stephen P.H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair A. Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Jamie A. Davies, Laura Amarosi, Catriona M.H. Anderson, Philip M. Beart, Stefan Broer, Paul A. Dawson, Gergely Gyimesi, Bruno Hagenbuch, James R. Hammond, Jules C. Hancox, Michal Hershfinkel, Ken‐ichi Inui, Yoshikatsu Kanai, Stephan Kemp, Edmund R.S. Kunji, Gavin Stewart, Sotiria Tavoulari, David T. Thwaites and Tiziano Verri 2023. The Concise Guide to PHARMACOLOGY 2023/24: Transporters. British Journal of Pharmacology. 180 (S2), pp. S374-S469. https://doi.org/10.1111/bph.16182

The Concise Guide to PHARMACOLOGY 2023/24: Catalytic receptors
Stephen P.H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair A. Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Jamie A. Davies, Annie Beuve, Peter Brouckaert, Clare Bryant, John C. Burnett, Richard W. Farndale, Andreas Friebe, John Garthwaite, Adrian J. Hobbs, Gavin E. Jarvis, Doris Koesling, Michaela Kuhn, David MacEwan, Tom P. Monie, Lincoln R. Potter, Michael Russwurm, Harald H.H.W. Schmidt, Johannes‐Peter Stasch, Scott A. Waldman and Mathie, A. 2023. The Concise Guide to PHARMACOLOGY 2023/24: Catalytic receptors. British Journal of Pharmacology. 180 (S2), pp. S241-S288. https://doi.org/10.1111/bph.16180

The Concise Guide to PHARMACOLOGY 2023/24: Enzymes
Stephen P.H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair A. Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Jamie A. Davies, Stephanie Annett, Detlev Boison, Kathryn Elisa Burns, Carmen Dessauer, Jurg Gertsch, Nuala Ann Helsby, Angelo A. Izzo, Rennolds Ostrom, Andreas Papapetropoulos, Nigel J. Pyne, Susan Pyne, Tracy Robson, Roland Seifert, Johannes‐Peter Stasch, Csaba Szabo, Mario van der Stelt, Albert van der Vliet, Val Watts, Szu Shen Wong and Mathie, A. 2023. The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. British Journal of Pharmacology. 180 (S2), pp. S289-S373. https://doi.org/10.1111/bph.16181

The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets
Stephen P. H. Alexander, Eamonn Kelly, Alistair A. Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, O. Peter Buneman, Elena Faccenda, Simon D. Harding, Michael Spedding, John A. Cidlowski, Doriano Fabbro, Anthony P. Davenport, Jörg Striessnig, Jamie A. Davies, Katelin E. Ahlers‐Dannen, Mohammed Alqinyah, Thiruma V. Arumugam, Christopher Bodle, Josephine Buo Dagner, Bandana Chakravarti, Shreoshi P. Choudhuri, Kirk M. Druey, Rory A. Fisher, Kyle J. Gerber, John R. Hepler, Shelley B. Hooks, Havish S. Kantheti, Behirda Karaj, Somayeh Layeghi‐Ghalehsoukhteh, Jae‐Kyung Lee, Zili Luo, Kirill Martemyanov, Luke D. Mascarenhas, Harrison McNabb, Carolina Montañez‐Miranda, Osita Ogujiofor, Hoa Phan, David L. Roman, Vincent Shaw, Benita Sjogren, Christopher Sobey, Mackenzie M. Spicer, Katherine E. Squires, Laurie Sutton, Menbere Wendimu, Thomas Wilkie, Keqiang Xie, Qian Zhang, Yalda Zolghadri and Mathie, A. 2023. The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets. British Journal of Pharmacology. 180 (S2), pp. S1-S22. https://doi.org/10.1111/bph.16176

The Concise Guide to PHARMACOLOGY 2023/24: Nuclear hormone receptors
Stephen P.H. Alexander, John A. Cidlowski, Eamonn Kelly, Alistair A. Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Jamie A. Davies, Laurel Coons, Peter J. Fuller, Kenneth S. Korach, Morag J. Young and Mathie, A. 2023. The Concise Guide to PHARMACOLOGY 2023/24: Nuclear hormone receptors. British Journal of Pharmacology. 180 (S2), pp. S223-S240. https://doi.org/10.1111/bph.16179

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors
Stephen P.H. Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair A. Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Jamie A. Davies, Maria Pia Abbracchio, George 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, Kenneth E. Bernstein, Bernhard Bettler, Nigel J.M. Birdsall, Victoria Blaho, Francois Boulay, Corinne Bousquet, Hans Bräuner‐Osborne, Geoffrey Burnstock, Girolamo Caló, Justo P. Castaño, Kevin J. Catt, Stefania Ceruti, Paul Chazot, Nan Chiang, Bice Chini, Jerold Chun, Antonia Cianciulli, Olivier Civelli, Lucie H. Clapp, Réjean Couture, Helen M. Cox, Zsolt Csaba, Claes Dahlgren, Gordon Dent, Steven D. Douglas, Pascal Dournaud, Satoru Eguchi, Emanuel Escher, Edward J. Filardo, Tung Fong, Marta Fumagalli, Raul R. Gainetdinov, Michael L. Garelja, Marc de Gasparo, Craig Gerard, Marvin Gershengorn, Fernand Gobeil, Theodore L. Goodfriend, Cyril Goudet, Lukas Grätz, Karen J. Gregory, Andrew L. Gundlach, Jörg Hamann, Julien Hanson, Richard L. Hauger, Debbie L. Hay, Akos Heinemann, Deron Herr, Morley D. Hollenberg, Nicholas D. Holliday, Mastgugu Horiuchi, Daniel Hoyer, László Hunyady, Ahsan Husain, Adriaan P. IJzerman, Tadashi Inagami, Kenneth A. Jacobson, Robert T. Jensen, Ralf Jockers, Deepa Jonnalagadda, Sadashiva Karnik, Klemens Kaupmann, Jacqueline Kemp, Charles Kennedy, Yasuyuki Kihara, Takio Kitazawa, Pawel Kozielewicz, Hans‐Jürgen Kreienkamp, Jyrki P. Kukkonen, Tobias Langenhan, Dan Larhammar, Katie Leach, Davide Lecca, John D. Lee, Susan E. Leeman, Jérôme Leprince, Xaria X. Li, Stephen J. Lolait, Amelie Lupp, Robyn Macrae, Janet Maguire, Davide Malfacini, 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, Tony Ngo, Xavier Norel, Duuamene Nyimanu, Anne‐Marie O’Carroll, Stefan Offermanns, Maria Antonietta Panaro, Marc Parmentier, Roger G. Pertwee, Jean‐Philippe Pin, Eric R. Prossnitz, Mark Quinn, Rithwik Ramachandran, Manisha Ray, Rainer K. Reinscheid, Philippe Rondard, G. Enrico Rovati, Chiara Ruzza, Gareth J. Sanger, Torsten Schöneberg, Gunnar Schulte, Stefan Schulz, Deborah L. Segaloff, Charles N. Serhan, Khuraijam Dhanachandra Singh, Craig M. Smith, Leigh A. Stoddart, Yukihiko Sugimoto, Roger Summers, Valerie P. Tan, David 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, Jean‐Pierre Vilardaga, Christopher S. Walker, Ji Ming Wang, Donald T. Ward, Hans‐Jürgen Wester, Gary B. Willars, Tom Lloyd Williams, Trent M. Woodruff, Chengcan Yao, Richard D. Ye and Mathie, A. 2023. The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. British Journal of Pharmacology. 180 (S2), pp. S23-S144. https://doi.org/10.1111/bph.16177

The Concise Guide to PHARMACOLOGY 2023/24: Ion channels
Stephen P. H. Alexander, Alistair A. Mathie, John A. Peters, Emma L. Veale, Jörg Striessnig, Eamonn Kelly, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Jamie A. Davies, Richard W. Aldrich, Bernard Attali, Austin M. Baggetta, Elvir Becirovic, Martin Biel, Roslyn M. Bill, Ana I. Caceres, William A. Catterall, Alex C. Conner, Paul Davies, Katrien De Clerq, Markus Delling, Francesco Di Virgilio, Simonetta Falzoni, Stefanie Fenske, Anna Fortuny‐Gomez, Samuel Fountain, Chandy George, Steve A. N. Goldstein, Christian Grimm, Stephan Grissmer, Kotdaji Ha, Verena Hammelmann, Israel Hanukoglu, Meiqin Hu, Ad P. Ijzerman, Sairam V. Jabba, Mike Jarvis, Anders A. Jensen, Sven E. Jordt, Leonard K. Kaczmarek, Stephan Kellenberger, Charles Kennedy, Brian King, Philip Kitchen, Qiang Liu, Joseph W. Lynch, Jessica Meades, Verena Mehlfeld, Annette Nicke, Stefan Offermanns, Edward Perez‐Reyes, Leigh D. Plant, Lachlan Rash, Dejian Ren, Mootaz M. Salman, Werner Sieghart, Lucia G. Sivilotti, Trevor G. Smart, Terrance P. Snutch, Jinbin Tian, James S. Trimmer, Charlotte Van den Eynde, Joris Vriens, Aguan D. Wei, Brenda T. Winn, Heike Wulff, Haoxing Xu, Fan Yang, Wei Fang, Lixia Yue, Xiaoli Zhang, Michael Zhu and Mathie, A. 2023. The Concise Guide to PHARMACOLOGY 2023/24: Ion channels. British Journal of Pharmacology. 180 (S2), pp. S145-S222. https://doi.org/10.1111/bph.16178

Aprepitant is a novel, selective activator of the K2P channel TRAAK
McCoull, D., Veall, E.L., Walsh, Y., Byrom, L., Avkiran, T., Large, J.M., Vaitone, E., Gaffey, F., Jerman, J., Mathie, A. and Wright, P.D. 2022. Aprepitant is a novel, selective activator of the K2P channel TRAAK. Biochemical and Biophysical Research Communications. 588, pp. 41-46. https://doi.org/10.1016/j.bbrc.2021.12.031

Gain and loss of TASK3 channel function and its regulation by novel variation cause KCNK9 imprinting syndrome
Cousin, M.A., Veale, E.L., Dsouza, N.R., Tripathi, S., Holden, R.G., Arelin, M., Beek, G., Bekheirnia, M.R., Beygo, J., Bhambhani, V., Bialer, M., Bigoni, S., Boelman, C., Klee, E.W. and Mathie, A. 2022. Gain and loss of TASK3 channel function and its regulation by novel variation cause KCNK9 imprinting syndrome. Genome Medicine. 14 62. https://doi.org/10.1186/s13073-022-01064-4

A KCNB1 gain of function variant causes developmental delay and speech apraxia but not seizures
Veale, E.L., Golluscio, A., Grand, K., Graham, J.M. Jr and Mathie, A. 2022. A KCNB1 gain of function variant causes developmental delay and speech apraxia but not seizures. Frontiers in Pharmacology. 13 1093313. https://doi.org/10.3389/fphar.2022.1093313

HIV and Schistosoma Co-Exposure Leads to Exacerbated Pulmonary Endothelial Remodeling and Dysfunction Associated with Altered Cytokine Landscape
Sandra Medrano-Garcia, Daniel Morales-Cano, Bianca Barreira, Alba Vera-Zambrano, Rahul Kumar, Djuro Kosanovic, Ralph Theo Schermuly, Brian B. Graham, Francisco Perez-Vizcaino, Alistair Mathie, Rajkumar Savai, Soni Pullamseti, Ghazwan Butrous, Edgar Fernández-Malavé and Angel Cogolludo 2022. HIV and Schistosoma Co-Exposure Leads to Exacerbated Pulmonary Endothelial Remodeling and Dysfunction Associated with Altered Cytokine Landscape. Cells. 11 (15) 2414. https://doi.org/10.3390/cells11152414

Heterologous Expression of Ion Channels in Mammalian Cell Lines
Mathie, A. 2021. Heterologous Expression of Ion Channels in Mammalian Cell Lines. in: Dallas, M. and Bell, D. (ed.) Patch Clamp Electrophysiology: Methods and Protocols Springer. pp. 51-65

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Ion channels
Stephen P.H. Alexander, Alistair Mathie, John A. Peters, Emma L. Veale, Jörg Striessnig, Eamonn Kelly, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Christopher Southan, Jamie A. Davies, Richard W. Aldrich, Bernard Attali, Austin M. Baggetta, Elvir Becirovic, Martin Biel, Roslyn M. Bill, William A. Catterall, Alex C. Conner, Paul Davies, Markus Delling, Francesco Di Virgilio, Simonetta Falzoni, Stefanie Fenske, Chandy George, Steve A.N. Goldstein, Stephan Grissmer, Kotdaji Ha, Verena Hammelmann, Israel Hanukoglu, Mike Jarvis, Anders A. Jensen, Leonard K. Kaczmarek, Stephan Kellenberger, Charles Kennedy, Brian King, Philip Kitchen, Joseph W. Lynch, Edward Perez‐Reyes, Leigh D. Plant, Lachlan Rash, Dejian Ren, Mootaz M. Salman, Lucia G. Sivilotti, Trevor G. Smart, Terrance P. Snutch, Jinbin Tian, James S. Trimmer, Charlotte Van den Eynde, Joris Vriens, Aguan D. Wei, Brenda T. Winn, Heike Wulff, Haoxing Xu, Lixia Yue, Xiaoli Zhang and Michael Zhu 2021. THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Ion channels. British Journal of Pharmacology. 178 (S1), pp. S157-S245. https://doi.org/10.1111/bph.15539

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Transporters
Stephen P.H. Alexander, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Christopher Southan, Jamie A. Davies, Laura Amarosi, Catriona M.H. Anderson, Philip Mark Beart, Stefan Broer, Paul A. Dawson, Bruno Hagenbuch, James R. Hammond, Jules C. Hancox, Ken‐ichi Inui, Yoshikatsu Kanai, Stephan Kemp, Gavin Stewart, David T. Thwaites and Tiziano Verri 2021. THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Transporters. British Journal of Pharmacology. 178 (S1), pp. S412-S513. https://doi.org/10.1111/bph.15543

The Concise Guide to Pharmacology 2021/22: G protein‐coupled receptors
Stephen P.H. Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Christopher Southan, Jamie A. Davies, Maria Pia Abbracchio, Wayne Alexander, Khaled Al‐hosaini, Magnus Bäck, Nicholas M. Barnes, Ross Bathgate, Jean‐Martin Beaulieu, Kenneth E. Bernstein, Bernhard Bettler, Nigel J.M. Birdsall, Victoria Blaho, Francois Boulay, Corinne Bousquet, Hans Bräuner‐Osborne, Geoffrey Burnstock, Girolamo Caló, Justo P. Castaño, Kevin J. Catt, Stefania Ceruti, Paul Chazot, Nan Chiang, Bice Chini, Jerold Chun, Antonia Cianciulli, Olivier Civelli, Lucie H. Clapp, Réjean Couture, Zsolt Csaba, Claes Dahlgren, Gordon Dent, Khuraijam Dhanachandra Singh, Steven D. Douglas, Pascal Dournaud, Satoru Eguchi, Emanuel Escher, Edward J. Filardo, Tung Fong, Marta Fumagalli, Raul R. Gainetdinov, Marc de Gasparo, Craig Gerard, Marvin Gershengorn, Fernand Gobeil, Theodore L. Goodfriend, Cyril Goudet, Karen J. Gregory, Andrew L. Gundlach, Jörg Hamann, Julien Hanson, Richard L. Hauger, Debbie L. Hay, Akos Heinemann, Morley D. Hollenberg, Nicholas D. Holliday, Mastgugu Horiuchi, Daniel Hoyer, László Hunyady, Ahsan Husain, Adriaan P. IJzerman, Tadashi Inagami, Kenneth A. Jacobson, Robert T. Jensen, Ralf Jockers, Deepa Jonnalagadda, Sadashiva Karnik, Klemens Kaupmann, Jacqueline Kemp, Charles Kennedy, Yasuyuki Kihara, Takio Kitazawa, Pawel Kozielewicz, Hans‐Jürgen Kreienkamp, Jyrki P. Kukkonen, Tobias Langenhan, Katie Leach, Davide Lecca, John D. Lee, Susan E. Leeman, Jérôme Leprince, Xaria X. Li, Tom Lloyd Williams, Stephen J. Lolait, Amelie Lupp, Robyn Macrae, Janet Maguire, Jean Mazella, Craig A. McArdle, Shlomo Melmed, Martin C. Michel, Laurence J. Miller, Vincenzo Mitolo, Bernard Mouillac, Christa E. Müller, Philip Murphy, Jean‐Louis Nahon, Tony Ngo, Xavier Norel, Duuamene Nyimanu, Anne‐Marie O’Carroll, Stefan Offermanns, Maria Antonietta Panaro, Marc Parmentier, Roger G. Pertwee, Jean‐Philippe Pin, Eric R. Prossnitz, Mark Quinn, Rithwik Ramachandran, Manisha Ray, Rainer K. Reinscheid, Philippe Rondard, G. Enrico Rovati, Chiara Ruzza, Gareth J. Sanger, Torsten Schöneberg, Gunnar Schulte, Stefan Schulz, Deborah L. Segaloff, Charles N. Serhan, Leigh A. Stoddart, Yukihiko Sugimoto, Roger Summers, Valerie P. Tan, David Thal, Walter (Wally) Thomas, Pieter B.M.W.M. Timmermans, Kalyan Tirupula, Giovanni Tulipano, Hamiyet Unal, Thomas Unger, Celine Valant, Patrick Vanderheyden, David Vaudry, Hubert Vaudry, Jean‐Pierre Vilardaga, Christopher S. Walker, Ji Ming Wang, Donald T. Ward, Hans‐Jürgen Wester, Gary B Willars, Trent M. Woodruff, Chengcan Yao and Richard D. Ye 2021. The Concise Guide to Pharmacology 2021/22: G protein‐coupled receptors. British Journal of Pharmacology. 178 (S1), pp. S27-S156. https://doi.org/10.1111/bph.15538

The Concise Guide to Pharmacology 2021/22: Introduction and Other Protein Targets
Stephen P H Alexander, Eamonn Kelly, Alistair Mathie, John A Peters, Emma L Veale, Jane F Armstrong, Elena Faccenda, Simon D Harding, Adam J Pawson, Christopher Southan, O Peter Buneman, John A Cidlowski, Arthur Christopoulos, Anthony P Davenport, Doriano Fabbro, Michael Spedding, Jörg Striessnig, Jamie A Davies, Katelin E. Ahlers‐Dannen, Mohammed Alqinyah, Thiruma V. Arumugam, Christopher Bodle, Josephine Buo Dagner, Bandana Chakravarti, Shreoshi P. Choudhuri, Kirk M. Druey, Rory A. Fisher, Kyle J. Gerber, John R. Hepler, Shelley B. Hooks, Havish S. Kantheti, Behirda Karaj, Somayeh Layeghi‐Ghalehsoukhteh, Jae‐Kyung Lee, Zili Luo, Kirill Martemyanov, Luke D. Mascarenhas, Harrison McNabb, Carolina Montañez‐Miranda, Osita Ogujiofor, Hoa Phan, David L. Roman, Vincent Shaw, Benita Sjogren, Christopher Sobey, Mackenzie M. Spicer, Katherine E. Squires, Laurie Sutton, Menbere Wendimu, Thomas Wilkie, Keqiang Xie, Qian Zhang and Yalda Zolghadri 2021. The Concise Guide to Pharmacology 2021/22: Introduction and Other Protein Targets. British Journal of Pharmacology. 178 (S1), pp. S1-S26. https://doi.org/10.1111/bph.15537

The Concise Guide to Pharmacology 2021/22: Enzymes
Stephen P.H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Christopher Southan, Jamie A. Davies, Stephanie Annett, Detlev Boison, Kathryn Elisa Burns, Carmen Dessauer, Jürg Gertsch, Nuala Ann Helsby, Angelo A. Izzo, Doris Koesling, Rennolds Ostrom, Andreas Papapetropoulos, Nigel J. Pyne, Susan Pyne, Tracy Robson, Michael Russwurm, Roland Seifert, Johannes‐Peter Stasch, Csaba Szabo, Mario van der Stelt, Albert van der Vliet, Val Watts and Szu Shen Wong 2021. The Concise Guide to Pharmacology 2021/22: Enzymes. British Journal of Pharmacology. 178 (S1), pp. S313-S411. https://doi.org/10.1111/bph.15542

The Concise Guide to Pharmacology 2021/22: Catalytic receptors
Stephen P.H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Christopher Southan, Jamie A. Davies, Annie Beuve, Peter Brouckaert, Clare Bryant, John C. Burnett, Richard W. Farndale, Andreas Friebe, John Garthwaite, Adrian J. Hobbs, Gavin E. Jarvis, Michaela Kuhn, David MacEwan, Tom P. Monie, Lincoln R. Potter, Harald H.H.W. Schmidt and Scott A. Waldman 2021. The Concise Guide to Pharmacology 2021/22: Catalytic receptors. British Journal of Pharmacology. 178 (S1), pp. S264-S312. https://doi.org/10.1111/bph.15541

The Concise Guide to Pharmacology 2021/22: Nuclear hormone receptors
Stephen P H Alexander, John A Cidlowski, Eamonn Kelly, Alistair Mathie, John A Peters, Emma L Veale, Jane F Armstrong, Elena Faccenda, Simon D Harding, Adam J Pawson, Christopher Southan, Jamie A Davies, Laurel Coons, Peter J. Fuller, Kenneth S. Korach and Morag J. Young 2021. The Concise Guide to Pharmacology 2021/22: Nuclear hormone receptors. British Journal of Pharmacology. 178 (S1), pp. S246-S263. https://doi.org/10.1111/bph.15540

Pharmacological Approaches to Studying Potassium Channels
Mathie, A. 2021. Pharmacological Approaches to Studying Potassium Channels. in: Nikita Gamper and KeWei Wang (ed.) Pharmacology of Potassium Channels Springer. pp. 83-111

Block of TREK and TRESK K2P channels by lamotrigine and two derivatives sipatrigine and CEN-092
Yvonne Walsh, Michael Leach, Emma L. Veale and Alistair Mathie 2021. Block of TREK and TRESK K2P channels by lamotrigine and two derivatives sipatrigine and CEN-092. Biochemistry and Biophysics Reports. 26. https://doi.org/10.1016/j.bbrep.2021.101021

A “Target Class” Screen to Identify Activators of Two-Pore Domain Potassium (K2P) Channels
Mathie, A. 2021. A “Target Class” Screen to Identify Activators of Two-Pore Domain Potassium (K2P) Channels. SLAS DISCOVERY: Advancing the Science of Drug Discovery. 26 (3), pp. 428-438. https://doi.org/10.1177/2472555220976126

Pharmacists detecting atrial fibrillation in general practice: a qualitative focus group study.
Savickas, V., Veale, E.L., Bhamra, S.K., Stewart, A.J., Mathie, A. and Corlett, S. 2020. Pharmacists detecting atrial fibrillation in general practice: a qualitative focus group study. BJGP Open. 4 (3) bjgpopen20X101042. https://doi.org/10.3399/bjgpopen20x101042

TASK-3 Two-Pore Potassium Channels drive neuronal excitability of the circadian clock and entrainment to challenging light environments
Aiste Steponenaite, Tatjana Lalic, Lynsey Atkinson, Liting Wei, Alistair Mathie, M. Zameel Cader and Gurprit S. Lall 2020. TASK-3 Two-Pore Potassium Channels drive neuronal excitability of the circadian clock and entrainment to challenging light environments. biorxiv.org. https://doi.org/10.1101/2020.07.27.222885

TRESK is a key regulator of nocturnal suprachiasmatic nucleus dynamics and light adaptive responses
Tatjana Lalic, Aiste Steponenaite, Liting Wei, Sridhar R. Vasudevan, Alistair Mathie, Stuart N. Peirson, Gurprit S. Lall and M. Zameel Cader 2020. TRESK is a key regulator of nocturnal suprachiasmatic nucleus dynamics and light adaptive responses. Nature Communications . 11 4614. https://doi.org/10.1038/s41467-020-17978-9

Opportunistic screening for atrial fibrillation by clinical pharmacists in UK general practice during the influenza vaccination season: A cross-sectional feasibility study.
Savickas, Vilius, Stewart, Adrian J., Rees-Roberts, Melanie, Short, Vanessa, Bhamra, Sukvinder K., Corlett, Sarah A., Mathie, A. and Veale, Emma L. 2020. Opportunistic screening for atrial fibrillation by clinical pharmacists in UK general practice during the influenza vaccination season: A cross-sectional feasibility study. PLoS Medicine. 17 (7) e1003197. https://doi.org/10.1371/journal.pmed.1003197

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Transporters
Stephen P.H. Alexander, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Joanna L. Sharman, Christopher Southan and Jamie A. Davies 2019. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Transporters. British Journal of Pharmacology. 176 (S1), pp. S397-S493. https://doi.org/10.1111/bph.14753

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Enzymes
Stephen P.H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Joanna L. Sharman, Christopher Southan and Jamie A. Davies 2019. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Enzymes. British Journal of Pharmacology. 176 (S1), pp. S297-S396. https://doi.org/10.1111/bph.14752

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors
Stephen P.H. Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Joanna L. Sharman, Christopher Southan and Jamie A. Davies 2019. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors. British Journal of Pharmacology. 176 (S1), pp. S21-S141. https://doi.org/10.1111/bph.14748

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Introduction and Other Protein Targets
Stephen P.H. Alexander, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Joanna L. Sharman, Christopher Southan, O. Peter Buneman, John A. Cidlowski, Arthur Christopoulos, Anthony P. Davenport, Doriano Fabbro, Michael Spedding, Jörg Striessnig and Jamie A. Davies 2019. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Introduction and Other Protein Targets. British Journal of Pharmacology. 176, pp. S1-S20. https://doi.org/10.1111/bph.14747

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Nuclear hormone receptors
Stephen P H Alexander, John A Cidlowski, Eamonn Kelly, Alistair Mathie, John A Peters, Emma L Veale, Jane F Armstrong, Elena Faccenda, Simon D Harding, Adam J Pawson, Joanna L Sharman, Christopher Southan and Jamie A Davies 2019. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Nuclear hormone receptors. British Journal of Pharmacology. https://doi.org/10.1111/bph.14750

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Catalytic receptors
Stephen P.H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Joanna L. Sharman, Christopher Southan and Jamie A. Davies 2019. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Catalytic receptors. British Journal of Pharmacology. 176, pp. S247-S296. https://doi.org/10.1111/bph.14751

The Concise Guide to Pharmacology 2019/20: Ion channels
Stephen P.H. Alexander, Alistair Mathie, John A. Peters, Emma L. Veale, Jörg Striessnig, Eamonn Kelly, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Joanna L. Sharman, Christopher Southan and Jamie A. Davies 2019. The Concise Guide to Pharmacology 2019/20: Ion channels. British Journal of Pharmacology. 176 (S1), pp. S142-S228. https://doi.org/10.1111/bph.14749

Editorial: Infection in pulmonary vascular diseases: Would another consortium really be the way to go?
Butrous, G. and Mathie, A. 2019. Editorial: Infection in pulmonary vascular diseases: Would another consortium really be the way to go? Global Cardiology Science & Practice. 2019 (1). https://doi.org/10.21542/gcsp.2019.1

Pharmacologically reversible, loss of function mutations in the TM2 and TM4 inner pore helices of TREK-1 K2P channels
Ehab Al-Moubarak, Emma L. Veale and Alistair Mathie 2019. Pharmacologically reversible, loss of function mutations in the TM2 and TM4 inner pore helices of TREK-1 K2P channels. Scientific Reports. 9 12394. https://doi.org/10.1038/s41598-019-48855-1

Characterization and regulation of wild‐type and mutant TASK‐1 two pore domain potassium channels indicated in pulmonary arterial hypertension
Cunningham, K.P., Holden, R.G., Escribano‐Subias, P.M., Cogolludo, A., Veale, E.L. and Mathie, A. 2019. Characterization and regulation of wild‐type and mutant TASK‐1 two pore domain potassium channels indicated in pulmonary arterial hypertension. Journal of Physiology. 597 (4), pp. 1087-1101. https://doi.org/10.1113/jp277275

GI-530159, a novel, selective, mechano-sensitive K2P channel opener, reduces rat dorsal root ganglion (DRG) neuron excitability
Alexandre J.C. Loucif, Pierre-Philippe Saintot, Jia Liu, Brett M. Antonio, Shannon G. Zellmer, Katrina Yoger, Emma L. Veale, Anna Wilbrey, Kiyoyuki Omoto, Lishuang Cao, Alex Gutteridge, Neil A. Castle, Edward B. Stevens and Alistair Mathie 2018. GI-530159, a novel, selective, mechano-sensitive K2P channel opener, reduces rat dorsal root ganglion (DRG) neuron excitability. British Journal of Pharmacology. 175 (12), pp. 2272-2283. https://doi.org/10.1111/bph.14098

HIV transgene expression impairs K+ channel function in the pulmonary vasculature
Mondejar-Parreño, G., Morales-Cano, D., Barreira, B., Callejo, M., Ruiz-Cabello, J., Moreno, L., Esquivel-Ruiz, S., Mathie, A., Butrous, G., Perez-Vizcaino, F. and Cogolludo, A. 2018. HIV transgene expression impairs K+ channel function in the pulmonary vasculature. American Journal of Physiology: Lung and Molecular Physiology. 315 (5), pp. L711-L723. https://doi.org/10.1152/ajplung.00045.2018

Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons.
Fernández-Fernández, D., Cadaveira-Mosquera, A., Rueda-Ruzafa, L., Herrera-Pérez, S., Veale, E.L., Reboreda, A., Mathie, A. and Lamas, J.A. 2018. Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons. PLoS ONE. 13 (6) e0199282. https://doi.org/10.1371/journal.pone.0199282

Pharmacists detecting atrial fibrillation (PDAF) in primary care during the influenza vaccination season: a multisite, cross-sectional screening protocol
Emma L Veale, Adrian J Stewart, Alistair Mathie, Satvinder K Lall, Melanie Rees-Roberts, Vilius Savickas, Sukvinder K Bhamra and Sarah A Corlett 2018. Pharmacists detecting atrial fibrillation (PDAF) in primary care during the influenza vaccination season: a multisite, cross-sectional screening protocol. BMJ Open. 8 (3) e021121. https://doi.org/10.1136/bmjopen-2017-021121

Terbinafine is a novel and selective activator of the two-pore domain potassium channel TASK3
Paul D. Wright, Emma L. Veale, David McCoull, David C. Tickle, Jonathan M. Large, Emma Ococks, Gemma Gothard, Catherine Kettleborough, Alistair Mathie and Jeffrey Jerman 2017. Terbinafine is a novel and selective activator of the two-pore domain potassium channel TASK3. Biochemical and Biophysical Research Communications. 493 (1), pp. 444-450. https://doi.org/10.1016/j.bbrc.2017.09.002

Enhanced inflammatory cell profiles in schistosomiasis-induced pulmonary vascular remodeling
Ali, Z., Kosanovic, D., Kolosionek, E., Schermuly, R.T., Graham, B.B., Mathie, A. and Butrous, G. 2017. Enhanced inflammatory cell profiles in schistosomiasis-induced pulmonary vascular remodeling. Pulmonary Circulation. 7 (1), pp. 244-252. https://doi.org/10.1086/690687

TASK-1 (KCNK3) channels in the lung: from cell biology to clinical implications
Andrea Olschewski, Emma L. Veale, Bence M. Nagy, Chandran Nagaraj, Grazyna Kwapiszewska, Fabrice Antigny, Mélanie Lambert, Marc Humbert, Gábor Czirják, Péter Enyedi and Alistair Mathie 2017. TASK-1 (KCNK3) channels in the lung: from cell biology to clinical implications. The European Respiratory Journal. 50 (5) 1700754. https://doi.org/10.1183/13993003.00754-2017

Aristolochic acid, a plant extract used in the treatment of pain and linked to Balkan Endemic Nephropathy, is a regulator of K2P channels
Veale, E.L. and Mathie, A. 2016. Aristolochic acid, a plant extract used in the treatment of pain and linked to Balkan Endemic Nephropathy, is a regulator of K2P channels. British Journal of Pharmacology. 173 (10), pp. 1639-1652. https://doi.org/10.1111/bph.13465

Two-pore domain potassium channels: Potential therapeutic targets for the treatment of pain
Mathie, A. and Veale, E.L. 2015. Two-pore domain potassium channels: Potential therapeutic targets for the treatment of pain. Pflügers Archiv - European Journal of Physiology. 467, pp. 931-943. https://doi.org/10.1007/s00424-014-1655-3

Influence of the N terminus on the biophysical properties and pharmacology of TREK1 potassium channels
Veale, E.L., Al-Moubarak, E., Bajaria, N., Omoto, K., Cao, L., Tucker, S.J., Stevens, E.B. and Mathie, A. 2014. Influence of the N terminus on the biophysical properties and pharmacology of TREK1 potassium channels. Molecular Pharmacology. 85 (5), pp. 671-681. https://doi.org/10.1124/mol.113.091199

Enhancement of TWIK-related acid-sensitive potassium channel 3 (TASK3) two-pore domain potassium channel activity by tumor necrosis factor α
El Hachmane, M.F., Rees, K.A., Veale, E.L., Sumbayev, V.V. and Mathie, A. 2014. Enhancement of TWIK-related acid-sensitive potassium channel 3 (TASK3) two-pore domain potassium channel activity by tumor necrosis factor α. Journal of Biological Chemistry. 289 (3), pp. P1388-1401. https://doi.org/10.1074/jbc.m113.500033

Recovery of current through mutated TASK3 potassium channels underlying birk barel syndrome
Veale, E.L., Hassan, M., Walsh, Y., Al-Moubarak, E. and Mathie, A. 2014. Recovery of current through mutated TASK3 potassium channels underlying birk barel syndrome. Molecular Pharmacology. 85 (3), pp. 397-407. https://doi.org/10.1124/mol.113.090530

Enhancement of Current through Trek1 Two Pore Domain Channels by Flufenamic Acid
Ehab Al-Moubarak and Alistair Mathie 2014. Enhancement of Current through Trek1 Two Pore Domain Channels by Flufenamic Acid. Biophysical Journal. 106 (2, supplement 1), p. 748A. https://doi.org/10.1016/j.bpj.2013.11.4121

GuideToPharmacology.org - An update
Alexander, S.P.H., Benson, H.E., Davenport, A., Mathie, A., McGrath, I.J.C., Pawson, A.J., Peters, J.A., Sharman, J.L., Spedding, M. and Harmar, A.J. 2012. GuideToPharmacology.org - An update. British Journal of Pharmacology. 167 (4), pp. 697-698. https://doi.org/10.1111/j.1476-5381.2012.02141.x

Guide to Receptors and Channels (GRAC), 5th edition
Alexander, S.P., Mathie, A. and Peters, J.A. 2011. Guide to Receptors and Channels (GRAC), 5th edition. British Journal of Pharmacology. 164 (S1). https://doi.org/10.1111/j.1476-5381.2011.01649_1.x

Ion channels as novel therapeutic targets in the treatment of pain
Mathie, A. 2010. Ion channels as novel therapeutic targets in the treatment of pain. Journal of Pharmacy and Pharmacology. 62 (9), pp. 1089-1095. https://doi.org/10.1111/j.2042-7158.2010.01131.x

Dominant negative effects of a non-conducting TREK1 splice variant expressed in brain
Veale, E.L., Rees, K.A., Mathie, A. and Trapp, S. 2010. Dominant negative effects of a non-conducting TREK1 splice variant expressed in brain. Journal of Biological Chemistry. 285 (38), pp. P29295-29304. https://doi.org/10.1074/jbc.m110.108423

Trafficking of neuronal two pore domain potassium channels
Mathie, A., Rees, K.A., El Hachmane, M.F. and Veale, E.L. 2010. Trafficking of neuronal two pore domain potassium channels. Current Neuropharmacology. 8 (3), pp. 276-286. https://doi.org/10.2174/157015910792246146

Symposium Review: Gating of two pore domain potassium channels
Mathie, A., Al-Moubarak, E. and Veale, E.L. 2010. Symposium Review: Gating of two pore domain potassium channels. Journal of Physiology. 588 (17), pp. 3149-3156. https://doi.org/10.1113/jphysiol.2010.192344

Guide to Receptors and Channels (GRAC), 4th edition
Alexander, S.P.H., Mathie, A. and Peters, J.A. 2009. Guide to Receptors and Channels (GRAC), 4th edition. British Journal of Pharmacology. 158 (S1). https://doi.org/10.1111/j.1476-5381.2009.00499.x

Neuronal Potassium Channels
Alistair Mathie and Emma L. Veale 2009. Neuronal Potassium Channels. in: Binder, M.D., Hirokawa, N. and Windhorst, U. (ed.) Encyclopedia of Neuroscience Springer Nature. pp. 2792–2797

Guide to Receptors and Channels (GRAC), 3rd edition
Alexander, S.P.H., Mathie, A. and Peters, J.A. 2008. Guide to Receptors and Channels (GRAC), 3rd edition. British Journal of Pharmacology. 153 (Suppl. 2), p. S1–S209. https://doi.org/10.1038/sj.bjp.0707746

The M1P1 loop of TASK3 K2P channels apposes the selectivity filter and influences channel function
Clarke, C.E., Veale, E.L., Wyse, K., Vandenberg, J.I. and Mathie, A. 2008. The M1P1 loop of TASK3 K2P channels apposes the selectivity filter and influences channel function. Journal of Biological Chemistry. 283 (25), pp. 16985-16992. https://doi.org/10.1074/jbc.m801368200

Neuronal two-pore-domain potassium channels and their regulation by G protein-coupled receptors
Mathie, A. 2007. Neuronal two-pore-domain potassium channels and their regulation by G protein-coupled receptors. Journal of Physiology. 278 (2), pp. 377-385. https://doi.org/10.1113/jphysiol.2006.121582

Guide to Receptors and Channels (GRAC), 2nd edition
Alexander, S.P.H., Mathie, A. and Peters, J.A. 2007. Guide to Receptors and Channels (GRAC), 2nd edition. British Journal of Pharmacology. 150 (S1). https://doi.org/10.1038/sj.bjp.0707199

Gαq-Mediated Regulation of TASK3 Two-Pore Domain Potassium Channels: The Role of Protein Kinase C
Veale, E.L., Kennard, L.E., Sutton, G.L., MacKenzie, G., Sandu, C. and Mathie, A. 2007. Gαq-Mediated Regulation of TASK3 Two-Pore Domain Potassium Channels: The Role of Protein Kinase C. Molecular Pharmacology. 71 (6), pp. 1666-1675. https://doi.org/10.1124/mol.106.033241

TASK-3 two-pore domain potassium channels enable sustained high-frequency firing in cerebellar granule neurons
Brickley, S.G., Aller, M.I., Sandu, C., Veale, E.L., Alder, F.G., Sambi, H., Mathie, A. and Wisden, W. 2007. TASK-3 two-pore domain potassium channels enable sustained high-frequency firing in cerebellar granule neurons. Journal of Neuroscience. 27 (35), pp. 9329-9340. https://doi.org/10.1523/jneurosci.1427-07.2007

Identification of a region in the TASK3 two pore domain potassium channel that is critical for its blockade by methanandamide
Veale, E.L., Buswell, R., Clarke, C.E. and Mathie, A. 2007. Identification of a region in the TASK3 two pore domain potassium channel that is critical for its blockade by methanandamide. British Journal of Pharmacology. 152 (5), pp. 778-786. https://doi.org/10.1038/sj.bjp.0707436

Therapeutic potential of neuronal two-pore domain potassium-channel modulators
Mathie, A. and Veale, E.L. 2007. Therapeutic potential of neuronal two-pore domain potassium-channel modulators. Current Opinion in Investigational Drugs. 8 (7), pp. 555-562.

The in Vivo Contributions of TASK-1-Containing Channels to the Actions of Inhalation Anesthetics, the α2 Adrenergic Sedative Dexmedetomidine, and Cannabinoid Agonists
Linden, A.-M., Aller, M.I., Leppä, E., Vekovischeva, O., Aitta-Aho, T., Veale, E.L., Mathie, A., Rosenberg, P., Wisden, W. and Korpi, E.R. 2006. The in Vivo Contributions of TASK-1-Containing Channels to the Actions of Inhalation Anesthetics, the α2 Adrenergic Sedative Dexmedetomidine, and Cannabinoid Agonists. Journal of Pharmacology and Experimental Therapeutics. 317 (2), pp. 615-626. https://doi.org/10.1124/jpet.105.098525

Zinc and copper: Pharmacological probes and endogenous modulators of neuronal excitability
Mathie, A., Sutton, G.L., Clarke, C.E. and Veale, E.L. 2006. Zinc and copper: Pharmacological probes and endogenous modulators of neuronal excitability. Pharmacology & Therapeutics. 111 (3), pp. 567-583. https://doi.org/10.1016/j.pharmthera.2005.11.004

Inhibition of the human two-pore domain potassium channel, TREK-1, by fluoxetine and its metabolite norfluoxetine
Kennard, L.E., Chumbley, J.R., Ranatunga, K.M., Armstrong, S.J., Veale, E.L. and Mathie, A. 2005. Inhibition of the human two-pore domain potassium channel, TREK-1, by fluoxetine and its metabolite norfluoxetine. British Journal of Pharmacology. 144, pp. 821-829. https://doi.org/10.1038/sj.bjp.0706068

Modifying the subunit composition of TASK channels alters the modulation of a leak conductance in cerebellar granule neurons
Aller, M.I., Veale, E.L., Linden, A.-M., Sandu, C., Schwaninger, M., Evans, L.J., Korpi, E.R., Mathie, A., Wisden, W. and Brickley, S.G. 2005. Modifying the subunit composition of TASK channels alters the modulation of a leak conductance in cerebellar granule neurons. Journal of Neuroscience. 25 (49), pp. 11455-11467. https://doi.org/10.1523/jneurosci.3153-05.2005

Two-Pore-Domain Channels Are a Novel Target for the Anesthetic Gases Xenon, Nitrous Oxide, and Cyclopropane
Gruss, M., Bushell, T.J., Bright, D.P., Lieb, W.R., Mathie, A. and Franks, N.P. 2004. Two-Pore-Domain Channels Are a Novel Target for the Anesthetic Gases Xenon, Nitrous Oxide, and Cyclopropane. Molecular Pharmacology. 65 (2), pp. 443-452. https://doi.org/10.1124/mol.65.2.443

Selective block of the human 2-P domain potassium channel, TASK-3, and the native leak potassium current, IKSO, by zinc
Clarke, C.E., Veale, E.L., Green, P.J., Meadows, H.J. and Mathie, A. 2004. Selective block of the human 2-P domain potassium channel, TASK-3, and the native leak potassium current, IKSO, by zinc. Journal of Physiology. 560 (1), pp. 51-62. https://doi.org/10.1113/jphysiol.2004.070292

Guide to receptors and channels. 1st edition (2005 revision)
Alexander, S.P., Mathie, A. and Peters, J.A. 2004. Guide to receptors and channels. 1st edition (2005 revision). British Journal of Pharmacology. 144 (S1). https://doi.org/10.1038/sj.bjp.0706158

The Two-Pore-Domain K+ Channels TREK-1 and TASK-3 Are Differentially Modulated by Copper and Zinc
Gruss, M., Mathie, A., Lieb, W.R. and Franks, N.P. 2004. The Two-Pore-Domain K+ Channels TREK-1 and TASK-3 Are Differentially Modulated by Copper and Zinc. Molecular Pharmacology. 66 (3), pp. 530-537.

What are the roles of the many different types of potassium channel expressed in cerebellar granule cells?
Mathie, A., Clarke, C.E., Ranatunga, K.M. and Veale, E.L. 2003. What are the roles of the many different types of potassium channel expressed in cerebellar granule cells? The Cerebellum. 2, pp. 11-25. https://doi.org/10.1080/14734220310015593

Neuronal ion channels and their sensitivity to extremely low frequency weak electric field effects.
Mathie, A., Kennard, L.E. and Veale, E.L. 2003. Neuronal ion channels and their sensitivity to extremely low frequency weak electric field effects. Radiation Protection Dosimetry. 106 (4), pp. 311-315. https://doi.org/10.1093/oxfordjournals.rpd.a006365

Inhibition of the potassium current IKSO, in cerebellar granule cells, by the inhibitors of MEK1 activation, PD 98059 and U 0126
Boyd, D.F. and Mathie, A. 2002. Inhibition of the potassium current IKSO, in cerebellar granule cells, by the inhibitors of MEK1 activation, PD 98059 and U 0126. Neuropharmacology. 42 (2), pp. 221-228. https://doi.org/10.1016/s0028-3908(01)00168-x

Pharmacological characterization of a non-inactivating outward current observed in mouse cerebellar Purkinje neurones.
Bushell, T., Clarke, C., Mathie, A. and Robertson, B. 2002. Pharmacological characterization of a non-inactivating outward current observed in mouse cerebellar Purkinje neurones. British Journal of Pharmacology. 135, pp. 705-712. https://doi.org/10.1038/sj.bjp.0704518

Background potassium channels move into focus
Mathie, A. and Clarke, C.E. 2002. Background potassium channels move into focus. Journal of Physiology. 542 (2), p. 334. https://doi.org/10.1113/jphysiol.2002.020008

Mammalian Two-Pore Domain Potassium Channels
Alistair Mathie and Brian Robertson 2001. Mammalian Two-Pore Domain Potassium Channels. Physiology News. 43. https://doi.org/10.36866/pn.43.5

TiPS nomenclature supplement 2001
Steve Alexander, Alistair Mathie, John Peters, Gillian MacKenzie and Adam Smith 2001. TiPS nomenclature supplement 2001. Trends in Pharmacological Sciences. 22 (s1). https://doi.org/10.1016/s0165-6147(01)80001-8

Inhibition of delayed rectifier K+ conductance in cultured rat cerebellar granule neurons by activation of calcium-permeable AMPA receptors
Jones, G., Boyd, D.F., Yeung, S.Y. and Mathie, A. 2000. Inhibition of delayed rectifier K+ conductance in cultured rat cerebellar granule neurons by activation of calcium-permeable AMPA receptors. European Journal of Neuroscience. 12 (3), pp. 935-944. https://doi.org/10.1046/j.1460-9568.2000.00983.x

Purinergic and muscarinic receptor activation activates a common calcium entry pathway in rat neocortical neurons and glial cells
Prothero, L.S., Mathie, A. and Richards, C.D. 2000. Purinergic and muscarinic receptor activation activates a common calcium entry pathway in rat neocortical neurons and glial cells. Neuropharmacology. 39 (10), pp. 1768-1778. https://doi.org/10.1016/s0028-3908(00)00013-7

A functional role for the two-pore domain potassium channel TASK-1 in cerebellar granule neurons
Millar, J.A., Barratt, L., Southan, A.P., Page, K.M., Fyffe, R.E., Robertson, B. and Mathie, A. 2000. A functional role for the two-pore domain potassium channel TASK-1 in cerebellar granule neurons. Proceedings of the National Academy of Sciences. 97 (7), pp. 3614-3618. https://doi.org/10.1073/pnas.97.7.3614

The role of Ca2+ stores in the muscarinic inhibition of the K+ current IK(SO) in neonatal rat cerebellar granule cells
Boyd, D.F., Millar, J.A., Watkins, C.S. and Mathie, A. 2000. The role of Ca2+ stores in the muscarinic inhibition of the K+ current IK(SO) in neonatal rat cerebellar granule cells. Journal of Physiology. 529 (2), pp. 321-331. https://doi.org/10.1111/j.1469-7793.2000.00321.x

Inhibition of neuronal KV potassium currents by the antidepressant drug, fluoxetine
Yeung, S.Y., Millar, J.A. and Mathie, A. 1999. Inhibition of neuronal KV potassium currents by the antidepressant drug, fluoxetine. British Journal of Pharmacology. 128 (7), pp. 1609-1615. https://doi.org/10.1038/sj.bjp.0702955

Voltage-activated potassium channels in mammalian neurons and their block by novel pharmacological agents
Mathie, A., Wooltorton, J.R.A. and Watkins, C.S. 1998. Voltage-activated potassium channels in mammalian neurons and their block by novel pharmacological agents. General Pharmacology: The Vascular System. 30 (1), pp. 13-24. https://doi.org/10.1016/s0306-3623(97)00034-7

Characterization of the hyperpolarization - Activated chloride current in dissociated rat sympathetic neurons
Clark, S., Jordt, S.-E., Jentsch, T.J. and Mathie, A. 1998. Characterization of the hyperpolarization - Activated chloride current in dissociated rat sympathetic neurons. Journal of Physiology. 506 (3), pp. 665-678. https://doi.org/10.1111/j.1469-7793.1998.665bv.x

Activation of group I metabotropic glutamate receptors elicits pH changes in cultured rat cortical glia and neurons
Amos, B.J., Mathie, A. and Richards, C.D. 1998. Activation of group I metabotropic glutamate receptors elicits pH changes in cultured rat cortical glia and neurons. Neuroscience. 86 (4), pp. 1109-1120. https://doi.org/10.1016/s0306-4522(98)00072-4

Inhibition by inorganic ions of a sustained calcium signal evoked by activation of mGlu5 receptors in rat cortical neurons and glia.
Prothero, L.S., Richards, C.D. and Mathie, A. 1998. Inhibition by inorganic ions of a sustained calcium signal evoked by activation of mGlu5 receptors in rat cortical neurons and glia. British Journal of Pharmacology. 125, pp. 1551-1561. https://doi.org/10.1038/sj.bjp.0702203

Is EAG the answer to the M-current?
Mathie, A. and Watkins, C.S. 1997. Is EAG the answer to the M-current? Trends in Neurosciences. 20 (1), p. 14. https://doi.org/10.1016/s0166-2236(96)20057-8

Book review: Ion Channels: Molecules in Action. Edited by D. J. Aidley and P. R. Stanfield . Pp. 340. Cambridge University Press, 1996. £17.95 paperback, ISBN 0521 49882 1. £50.00 hardback, ISBN 0 521 49531 8
Alistair Mathie 1997. Book review: Ion Channels: Molecules in Action. Edited by D. J. Aidley and P. R. Stanfield . Pp. 340. Cambridge University Press, 1996. £17.95 paperback, ISBN 0521 49882 1. £50.00 hardback, ISBN 0 521 49531 8. Experimental Physiology. 109 (4), pp. 607-608. https://doi.org/10.1113/expphysiol.1998.sp004327

A non-inactivating K+ current sensitive to muscarinic receptor activation in rat cultured cerebellar granule neurons.
Watkins, C.S. and Mathie, A. 1996. A non-inactivating K+ current sensitive to muscarinic receptor activation in rat cultured cerebellar granule neurons. Journal of Physiology. 491 (2), pp. 401-412. https://doi.org/10.1113/jphysiol.1996.sp021224

Effects on K+ currents in rat cerebellar granule neurones of a membrane-permeable analogue of the calcium chelator BAPTA
Watkins, C.S. and Mathie, A. 1996. Effects on K+ currents in rat cerebellar granule neurones of a membrane-permeable analogue of the calcium chelator BAPTA. British Journal of Pharmacology. 118 (7), pp. 1772-1778. https://doi.org/10.1111/j.1476-5381.1996.tb15603.x

A non-inactivating K+ current sensitive to muscarinic receptor activation in rat cultured cerebellar granule neurons
Watkins, C.S. and Mathie, A. 1996. A non-inactivating K+ current sensitive to muscarinic receptor activation in rat cultured cerebellar granule neurons. Journal of Physiology. 491 (2), pp. 401-412. https://doi.org/10.1113/jphysiol.1996.sp021224

Book review: Methods in neurosciences volume 19: Ion channels of excitable cells
Mathie, A. 1995. Book review: Methods in neurosciences volume 19: Ion channels of excitable cells. Neuroscience. 64 (3), p. 845. https://doi.org/10.1016/0306-4522(95)90003-9

Multiple G-protein-coupled pathways inhibit N-type Ca channels of neurons
Hille, B., Beech, D.J., Bernheim, L., Mathie, A., Shapiro, M.S. and Wollmuth, L.P. 1995. Multiple G-protein-coupled pathways inhibit N-type Ca channels of neurons. Life Sciences. 56 (11-12), pp. 989-992. https://doi.org/10.1016/0024-3205(95)00038-8

Potent block of potassium currents in rat isolated sympathetic neurones by the uncharged form of amitriptyline and related tricyclic compounds
Wooltorton, J.R. and Mathie, A. 1995. Potent block of potassium currents in rat isolated sympathetic neurones by the uncharged form of amitriptyline and related tricyclic compounds. British Journal of Pharmacology. 116 (4), pp. 2191-2200. https://doi.org/10.1111/j.1476-5381.1995.tb15053.x

Erratum: Block of potassium currents in rat isolated sympathetic neurones by tricyclic antidepressants and structurally related compounds (Br. J. Pharmacol. (1993), 110, 1126-1132)
Wooltorton, J.R.A. and Mathie, A. 1994. Erratum: Block of potassium currents in rat isolated sympathetic neurones by tricyclic antidepressants and structurally related compounds (Br. J. Pharmacol. (1993), 110, 1126-1132). British Journal of Pharmacology. 111 (1), p. 377.

Modulation of the gating of the transient outward potassium current of rat isolated cerebellar granule neurons by lanthanum
Watkins, C.S. and Mathie, A. 1994. Modulation of the gating of the transient outward potassium current of rat isolated cerebellar granule neurons by lanthanum. Pflügers Archiv - European Journal of Physiology. 428, pp. 209-216. https://doi.org/10.1007/bf00724499

The modulation by lanthanum of the gating of voltage-dependent potassium currents in rat isolated cerebellar granule neurones
Watkins, C.S. and Mathie, A. 1993. The modulation by lanthanum of the gating of voltage-dependent potassium currents in rat isolated cerebellar granule neurones. Journal of Physiology. 473, p. 160P.

Block of potassium currents in rat isolated sympathetic neurones by tricyclic antidepressants and structurally related compounds
Wooltorton, J.R. and Mathie, A. 1993. Block of potassium currents in rat isolated sympathetic neurones by tricyclic antidepressants and structurally related compounds. British Journal of Pharmacology. 110 (3), pp. 1126-1132. https://doi.org/10.1111/j.1476-5381.1993.tb13931.x

5‐HT3 receptor channels in dissociated rat superior cervical ganglion neurons
Yang, J., Mathie, A. and Hille, B. 1992. 5‐HT3 receptor channels in dissociated rat superior cervical ganglion neurons. Journal of Physiology. 448 (1), pp. 237-256. https://doi.org/10.1113/jphysiol.1992.sp019039

Classification of muscarinic receptors inhibiting calcium current and M current in dissociated rat superior cervical ganglion (SCG) neurons
Mathie, A., Bernheim, L. and Hille, B. 1992. Classification of muscarinic receptors inhibiting calcium current and M current in dissociated rat superior cervical ganglion (SCG) neurons. Journal of Physiology. 446, p. 548P.

Inhibition of N- and L-type calcium channels by muscarinic receptor activation in rat sympathetic neurons
Mathie, A., Bernheim, L. and Hille, B. 1992. Inhibition of N- and L-type calcium channels by muscarinic receptor activation in rat sympathetic neurons. Neuron. 8 (5), pp. P907-914. https://doi.org/10.1016/0896-6273(92)90205-r

Characterization of muscarinic receptor subtypes inhibiting Ca2+ current and M current in rat sympathetic neurons
Bernheim, L., Mathie, A. and Hille, B. 1992. Characterization of muscarinic receptor subtypes inhibiting Ca2+ current and M current in rat sympathetic neurons. Proceedings of the National Academy of Sciences. 89 (20), pp. 9544-9548. https://doi.org/10.1073/pnas.89.20.9544

Conductance and kinetic properties of single nicotinic acetylcholine receptor channels in rat sympathetic neurones
Mathie, A., Cull‐Candy, S.G. and Colquhoun, D. 1991. Conductance and kinetic properties of single nicotinic acetylcholine receptor channels in rat sympathetic neurones. Journal of Physiology. 439 (1), pp. 717-750. https://doi.org/10.1113/jphysiol.1991.sp018690

Activation of glutamate receptors and glutamate uptake in identified macroglial cells in rat cerebellar cultures.
Wyllie, D.J., Mathie, A., Symonds, C.J. and Cull‐Candy, S.G. 1991. Activation of glutamate receptors and glutamate uptake in identified macroglial cells in rat cerebellar cultures. Journal of Physiology. 432 (1), pp. 235-258. https://doi.org/10.1113/jphysiol.1991.sp018383

Intracellular Ca2+ buffers disrupt muscarinic suppression of Ca2+ current and M current in rat sympathetic neurons
Beech, D.J., Bernheim, L., Mathie, A. and Hille, B. 1991. Intracellular Ca2+ buffers disrupt muscarinic suppression of Ca2+ current and M current in rat sympathetic neurons. Proceedings of the National Academy of Sciences. 88 (2), pp. 652-656. https://doi.org/10.1073/pnas.88.2.652

Function of nicotinic synapses
Colquhoun, D., Cachelin, A.B., Marshall, C.G., Mathie, A. and Ogden, D.C. 1990. Function of nicotinic synapses. in: Aquilonius, S-M. and Gillberg, P-G. (ed.) Cholinergic neurotransmission: functional and clinical aspects. Proceedings of Nobel Symposium 76. Lidingö Island, Stockholm, August 1989 Elsevier. pp. 43-50

Rectification of currents activated by nicotinic acetylcholine receptors in rat sympathetic ganglion neurones.
Mathie, A., Colquhoun, D. and Cull‐Candy, S.G. 1990. Rectification of currents activated by nicotinic acetylcholine receptors in rat sympathetic ganglion neurones. Journal of Physiology. 427 (1), pp. 625-655. https://doi.org/10.1113/jphysiol.1990.sp018191

Studies on single acetylcholine-receptor channels in muscle end-plate and sympathetic neurones
Colquhoun, D., Mathie, A., Mulrine, N.K. and Ogden, D.C. 1989. Studies on single acetylcholine-receptor channels in muscle end-plate and sympathetic neurones. Fernstrom Foundation Series. 13, pp. 217-234.

Acetylcholine receptor channels and their block by clonidine in cultured bovine chromaffin cells.
Cull‐Candy, S.G., Mathie, A. and Powis, D.A. 1988. Acetylcholine receptor channels and their block by clonidine in cultured bovine chromaffin cells. Journal of Physiology. 402 (1), pp. 255-278. https://doi.org/10.1113/jphysiol.1988.sp017203

Nicotinic acetylcholine receptors of nerve and muscle: Functional aspects
David Colquhoun, David C. Ogden and Alistair Mathie 1987. Nicotinic acetylcholine receptors of nerve and muscle: Functional aspects. Trends in Pharmacological Sciences. 8 (12), pp. 465-472. https://doi.org/10.1016/0165-6147(87)90040-x

Single-channel and whole-cell currents evoked by acetylcholine in dissociated sympathetic neurons of the rat
Mathie, A., Cull-Candy, S.G. and Colquhoun, D. 1987. Single-channel and whole-cell currents evoked by acetylcholine in dissociated sympathetic neurons of the rat. Proceedings of the Royal Society B: Biological Sciences. 232 (1267), pp. 239-248. https://doi.org/10.1098/rspb.1987.0072

Interactions between the effects of yohimbine, clonidine and [Ca]o on the electrical response of the mouse vas deferens
Blakeley, A.G., Mathie, A. and Petersen, S.A. 1986. Interactions between the effects of yohimbine, clonidine and [Ca]o on the electrical response of the mouse vas deferens. British Journal of Pharmacology. 88 (4), pp. 807-814. https://doi.org/10.1111/j.1476-5381.1986.tb16253.x

Ion channels activated by acetylcholine and gamma-aminobutyric acid in freshly dissociated sympathetic neurones of the rat.
Cull-Candy, S.G. and Mathie, A. 1986. Ion channels activated by acetylcholine and gamma-aminobutyric acid in freshly dissociated sympathetic neurones of the rat. Neuroscience Letters. 66 (3), pp. 275-280. https://doi.org/10.1016/0304-3940(86)90031-5

Alpha-adrenoceptors and facilitation at a sympathetic neuroeffector junction
Blakeley, A.G., Cunnane, T.C., Maskell, T., Mathie, A. and Petersen, S.A. 1984. Alpha-adrenoceptors and facilitation at a sympathetic neuroeffector junction. Journal of Autonomic Pharmacology. 4 (1), pp. 53-58. https://doi.org/10.1111/j.1474-8673.1984.tb00433.x

Facilitation at single release sites of a sympathetic neuroeffector junction in the mouse.
Blakeley, A.G., Mathie, A. and Petersen, S.A. 1984. Facilitation at single release sites of a sympathetic neuroeffector junction in the mouse. Journal of Physiology. 349 (1), pp. 57-71. https://doi.org/10.1113/jphysiol.1984.sp015142

Permalink - https://westminsterresearch.westminster.ac.uk/item/w9294/pranlukast-is-a-novel-small-molecule-activator-of-the-two-pore-domain-potassium-channel-trek2


Share this

Usage statistics

23 total views
13 total downloads
These values cover views and downloads from WestminsterResearch and are for the period from September 2nd 2018, when this repository was created.