Results 21 to 30 of about 3,728 (241)

Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [PDF]

Pharmacol Res Perspect, 2021
Unbound concentrations of of 14 commercial drugs in rat liver, muscle, and blood Abstract The unbound concentrations of 14 commercial drugs, including five non‐efflux/uptake transporter substrates—Class I, five efflux transporter substrates—class II and four influx transporter substrates—Class III, were simultaneously measured in rat liver, muscle, and
Wang S, Chen C, Guan C, Qiu L, Zhang L, Zhang S, Zhou H, Du H, Li C, Wu Y, Chang H, Wang T.   +11 more
europepmc   +2 more sources

Positive chronotropic action of HCN channel antagonism in human collecting lymphatic vessels. [PDF]

Physiol Rep, 2022
Hyperpolarisation‐activated cyclic‐nucleotide gated (HCN) channels primarily determine sinoatrial pacemaking. In human lymphatic vessels HCN channel proteins are also expressed but have a negligible functional role in ex vivo phasic activity when investigated using the HCN inhibitors ivabradine, ZD7288 and caesium.
Majgaard J, Skov FG, Kim S, Hjortdal VE, Boedtkjer DMB.   +4 more
europepmc   +2 more sources

The role of endocardial endothelium in the effect of histamine on myocardial contractions of histamine H1 and H2 receptor blockade [PDF]

Praxis Medica, 2016
Endocardial endothelium (EE) is a barrier which controls the passage of macromolecules and fluids between the blood and the adjacent miocardial interstitium. At the same time it is the place of synthesis of numerous endothelial mediators. Histamine as an
Smiljić Sonja, Parlić Dragica, Milanović Zvezdan, Nestorović Vojkan, Pavlović Mirjana   +4 more
doaj   +1 more source

Analytical and Pharmacological Characterization of 1-(Furan-2-Carbonyl)-LSD (1F-LSD) and Comparison With 1-(Thiophene-2-Carbonyl)-LSD (1T-LSD). [PDF]

Drug Test Anal
The novel lysergamide 1‐(furan‐2‐carbonyl)‐LSD (1F‐LSD) was analytically characterized. 1F‐LSD showed LSD‐like activity in vivo similar to 1‐(thiophene‐2‐carbonyl)‐LSD (1T‐LSD) used for comparison. Administration studies in mice and LC–MS analysis revealed that 1F‐LSD served as a prodrug.
Brandt SD, Kavanagh PV, Gare S, Elliott SP, Stratford A, Halberstadt AL.   +5 more
europepmc   +2 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

Association of Inpatient Prescribing of First-Generation Antihistamines With Delirium in Older Adults: A Cross-Sectional Study. [PDF]

J Am Geriatr Soc
ABSTRACT Background Small studies have reported associations between first‐generation antihistamines and delirium. It is unclear whether first‐generation antihistamines cause clinically important delirium among older adult inpatients. Objective To estimate the association between inpatient physician prescribing of first‐generation antihistamines and ...
Bridgman AC, Imrit MA, Roberts SB, Tadrous M, Stall NM, Fralick M, Watt J, Verma AA, Razak F, Drucker AM.   +9 more
europepmc   +2 more sources

Allergen‐free extracts from birch, ragweed, and hazel pollen activate human and guinea‐pig submucous and spinal sensory neurons

Neurogastroenterology &Motility, Volume 35, Issue 7, July 2023., 2023
Low molecular extracts from birch, ragweed, and hazel pollen strongly excite enteric and DRG neurons. Nerve activation was mediated by histamine in birch and ragweed, but not in hazel pollen extracts. Abstract Background Non‐allergenic, low molecular weight components of pollen grains are suspected to trigger changes in gut functions, sometimes leading
Sabine Buhner, Stefanie Schäuffele, Pieter Giesbertz, Ihsan Ekin Demir, Florian Zeller, Claudia Traidl‐Hoffmann, Michael Schemann, Stefanie Gilles   +7 more
wiley   +1 more source

The transport function of the human lymphatic system—A systematic review

Physiological Reports, Volume 11, Issue 11, June 2023., 2023
Abstract Physiological properties and function of the lymphatic system is still somewhat of a mystery. We report the current knowledge about human lymphatic vessel contractility and capability of adaptation. A literature search in PubMed identified studies published January 2000–September 2022.
Lene Thorup, Anders Hjortdal, Donna B. Boedtkjer, Morten B. Thomsen, Vibeke Hjortdal   +4 more
wiley   +1 more source

Critical role of mitogen‐inducible gene 6 in restraining endothelial cell permeability to maintain vascular homeostasis

Journal of Cell Communication and Signaling, Volume 17, Issue 1, Page 151-165, March 2023., 2023
Graphical abstract Xing et al. (2022) investigated the critical role of MIG6 in vascular permeability. MIG6 deficiency promotes VEGFA‐induced vascular permeability via activation of PLCγ1‐Ca2+‐eNOS signaling and perturbation of the balance in RAC1/RHOA activation, resulting in endothelial barrier disruption.
Liying Xing, Guanqun Huang, Rongyuan Chen, Lijuan Huang, Juanxi Liu, Xiangrong Ren, Shasha Wang, Haiqing Kuang, Anil Kumar, Jong Kyong Kim, Qin Jiang, Xuri Li, Chunsik Lee   +12 more
wiley   +1 more source