Results 1 to 10 of about 4,488 (204)

Structure of the dopamine D2 receptor in complex with the antipsychotic drug spiperone [PDF]

Nature Communications, 2020
統合失調症に関わるドパミン受容体の構造解明 --副作用を抑えた薬の迅速な探索・設計が可能に--. 京都大学プレスリリース. 2020-12-24.In addition to the serotonin 5-HT2A receptor (5-HT2AR), the dopamine D2 receptor (D2R) is a key therapeutic target of antipsychotics for the treatment of schizophrenia. The inactive
Aoki, Junken, Asada, Hidetsugu, Fujiwara, Takaaki, Im, Dohyun, Inoue, Asuka, Iwata, So, Kadji, Francois Marie Ngako, Kimura Terakado, Kanako, Mori, Chihiro, Nakane, Takanori, Nango, Eriko, Nomura, Norimichi, Shiimura, Yuki, Shimamura, Tatsuro, Tanaka, Tomoyuki, Tono, Kensuke, Uemura, Tomoko, Yamanaka, Yasuaki, Yamashita, Ayumi   +18 more
core   +10 more sources

Dissecting the Mechanism of Action of Spiperone— A Candidate for Drug Repurposing for Colorectal Cancer [PDF]

Cancers, 2022
Approximately 50% of colorectal cancer (CRC) patients still die from recurrence and metastatic disease, highlighting the need for novel therapeutic strategies. Drug repurposing is attracting increasing attention because, compared to traditional de novo drug discovery processes, it may reduce drug development periods and costs.
Cora', D., D'Alfonso, S., Genazzani, A.
core   +9 more sources

Micellar Hyaluronidase and Spiperone as a Potential Treatment for Pulmonary Fibrosis [PDF]

International Journal of Molecular Sciences, 2021
Concentration of hyaluronic acid (HA) in the lungs increases in idiopathic pulmonary fibrosis (IPF). HA is involved in the organization of fibrin, fibronectin, and collagen. HA has been proposed to be a biomarker of fibrosis and a potential target for antifibrotic therapy.
Evgenii Skurikhin, Pavel Madonov, Olga Pershina, Natalia Ermakova, Angelina Pakhomova, Darius Widera, Edgar Pan, Mariia Zhukova, Lubov Sandrikina, Andrey Artamonov, Alexander Dygai   +10 more
europepmc   +6 more sources

Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway [PDF]

BMC Pharmacology, 2009
Wnt signaling affects fundamental development pathways by regulating cell proliferation and differentiation. Aberrant activation of Wnt/beta-catenin signaling promotes the development of several cancers and is an attractive target for chemopreventive and chemotherapeutic agents.In order to identify the novel antagonists for the Wnt/beta-catenin pathway,
AD Kohn, AL Gundlach, C Liu, CH Park, D Lu, D Lu, DC Slusarski, Dennis A Carson, Desheng Lu, G Li, GP Reynolds, H Clevers, HY Meltzer, JE Leysen, JE Leysen, K Willert, L Liang, L Pani, LC Sheldahl, M Kuhl, M Kuhl, O Thastrup, P Maye, PG Strange, R Nusse, RJ Sharpe, RT Moon, SH Snyder, T Fukuda, Y Itzhak   +29 more
core   +6 more sources

Examining the effects of sodium ions on the binding of antagonists to dopamine D2 and D3 receptors [PDF]

PLoS ONE, 2016
Many G protein-coupled receptors have been shown to be sensitive to the presence of sodium ions (Na+). Using radioligand competition binding assays, we have examined and compared the effects of sodium ions on the binding affinities of a number of ...
A Malmberg, A Malmberg, A Wise, Alessio Lodola, BP Ceresa, BS Tsai, C Heidbreder, C Missale, CA Heidbreder, CB Pert, Claire L. Newton, DA Horstman, E Akam, EY Chien, HJ Motulsky, J Selent, JA Ballesteros, JA Javitch, JA Schetz, JC Schwartz, JP Overington, KA Neve, KA Neve, KA Neve, KA Neve, LE Limbird, M Michino, Martyn D. Wood, MM Teeter, OH Lowry, P Sokoloff, PG Strange, Philip G. Strange, RR Goodman, SS Ericksen, V Katritch, VA Boundy, Y Cordeaux   +37 more
core   +23 more sources

Spiperone: evidence for uptake into secretory granules. [PDF]

Proceedings of the National Academy of Sciences, 1984
Spiperone, a dopamine antagonist widely used as a specific ligand for dopamine and serotonin receptors, is actively accumulated into the F4C1 strain of rat pituitary tumor cells. The accumulation of 10 nM [3H]spiperone was linear for 3 min and reached a steady state after 10 min.
Priscilla S. Dannies, Hana Fishkes, Gary Rudnick, Marla S. Rudnick   +3 more
openaire   +4 more sources

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors

British Journal of Pharmacology, Volume 180, Issue S2, Page S23-S144, October 2023., 2023
The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands.
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   +165 more
wiley   +1 more source

Improved PIEZO1 agonism through 4‐benzoic acid modification of Yoda1

British Journal of Pharmacology, Volume 180, Issue 16, Page 2039-2063, August 2023., 2023
Background and Purpose The protein PIEZO1 forms mechanically activated, calcium‐permeable, non‐selective cation channels in numerous cell types from several species. Options for pharmacological modulation are limited and so we modified a small‐molecule agonist at PIEZO1 channels (Yoda1) to increase the ability to modulate these channels.
Gregory Parsonage, Kevin Cuthbertson, Naima Endesh, Nicoletta Murciano, Adam J. Hyman, Charlotte H. Revill, Oleksandr V. Povstyan, Eulashini Chuntharpursat‐Bon, Marjolaine Debant, Melanie J. Ludlow, Timothy Simon Futers, Laeticia Lichtenstein, Jacob A. Kinsella, Fiona Bartoli, Maria Giustina Rotordam, Nadine Becker, Andrea Brüggemann, Richard Foster, David J. Beech   +18 more
wiley   +1 more source

Chewing the fat: How lipidomics is changing our understanding of human health and disease in 2022

Analytical Science Advances, Volume 4, Issue 3-4, Page 104-131, May 2023., 2023
Abstract Lipids are biological molecules that play vital roles in all living organisms. They perform many cellular functions, such as 1) forming cellular and subcellular membranes, 2) storing and using energy, and 3) serving as chemical messengers during intra‐ and inter‐cellular signal transduction.
Caroline Géhin, Stephen J. Fowler, Drupad K. Trivedi   +2 more
wiley   +1 more source

Myopia control in Mendelian forms of myopia

Ophthalmic and Physiological Optics, Volume 43, Issue 3, Page 494-504, May 2023., 2023
Abstract Purpose To study the effectiveness of high‐dose atropine for reducing eye growth in Mendelian myopia in children and mice. Methods We studied the effect of high‐dose atropine in children with progressive myopia with and without a monogenetic cause. Children were matched for age and axial length (AL) in their first year of treatment.
Emilie van der Sande, Jan Roelof Polling, J. Willem L. Tideman, Magda A. Meester‐Smoor, Alberta A. H. J. Thiadens, Emily Tan, Chris I. De Zeeuw, Ralph Hamelink, Ingo Willuhn, Virginie J. M. Verhoeven, Beerend H. J. Winkelman, Caroline C. W. Klaver   +11 more
wiley   +1 more source