Results 61 to 70 of about 556,376 (281)

The Allosteric Mechanism of G‐Protein‐Coupled Receptors is Induced Fit, Not Conformational Selection

BioEssays, EarlyView.
Allosteric signaling of G‐protein‐coupled receptors (GPCRs) involves a population shift from inactive to active receptor conformations upon binding of ligand agonists. Kinetic and structural data indicate that this population shift is induced by ligand binding to inactive receptor conformations prior to the conformational change from inactive to active.
Kazem Asadollahi, Paul R. Gooley, Thomas R. Weikl   +2 more
wiley   +1 more source

Clinical potential of aclidinium bromide in chronic obstructive pulmonary disease

Therapeutics and Clinical Risk Management, 2014
Jun Zhong, Michael Roth Pneumology and Pulmonary Cell Research, Department of Biomedicine and Internal Medicine, University Hospital Basel, Basel, Switzerland Abstract: Chronic obstructive pulmonary disease (COPD) is increasing worldwide and is ...
Zhong J, Roth M
doaj  

Executive summary: Japanese guidelines for adult asthma (JGL) 2021

Allergology International, 2023
Asthma is characterized by chronic airway inflammation, variable airway narrowing, and sensory nerve irritation, which manifest as wheezing, dyspnea, chest tightness, and cough.
Akio Niimi, Koichi Fukunaga, Masami Taniguchi, Yoichi Nakamura, Etsuko Tagaya, Takahiko Horiguchi, Akihito Yokoyama, Masao Yamaguchi, Makoto Nagata   +8 more
doaj   +1 more source

Endothelium‐Independent Relaxation of Alkaloid Boldine in Isolated Aortas From Normotensive and Hypertensive Rats: Participation of Ca2+ Channels

Chemistry &Biodiversity, EarlyView.
Involvement of Ca2+ channels in boldine‐induced vascular relaxation. ABSTRACT The regulation of vascular tone plays a fundamental role in blood pressure homeostasis and still represents a significant challenge in clinical practice. Boldine, a naturally occurring alkaloid from Peumus boldus, has emerged as a compound of interest due to its therapeutic ...
Martina Odebrecht Cavichiolo, Rita de Cássia Vilhena da Silva, Valdir Cechinel Filho, Priscila de Souza   +3 more
wiley   +1 more source

The Forefront for Novel Therapeutic Agents Based on the Pathophysiology of Lower Urinary Tract Dysfunction: Ameliorative Effect of Solifenacin Succinate (Vesicare ®), a Bladder-Selective Antimuscarinic Agent, on Overactive Bladder Symptoms, Especially Urgency Episodes

Journal of Pharmacological Sciences, 2010
Overactive bladder (OAB) syndrome is a common condition that is most often observed in the elderly. Pharmacological treatment with muscarinic receptor antagonists has been most widely used for OAB. An antimuscarinic agent, solifenacin, showed the highest
Akiyoshi Ohtake, Shuichi Sato, Masao Sasamata, Keiji Miyata   +3 more
doaj   +1 more source

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of 18F‐Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3

ChemMedChem, EarlyView.
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Miguel A. Herrera‐Rueda, Maxwell A. Boateng, Melinda Wuest, Frederick G. West, Frank Wuest   +4 more
wiley   +1 more source

The effects of oral administration of the novel muscarinic receptor antagonist DA-8010 on overactive bladder in rat with bladder outlet obstruction

BMC Urology, 2020
Background DA-8010 is a novel compound developed for the treatment of overactive bladder (OAB) and urinary incontinence. The aims of this study were to investigate the effects of DA-8010 on OAB in a rat model.
Jin Bong Choi, Seung Hwan Jeon, Eun Bi Kwon, Woong Jin Bae, Hyuk Jin Cho, U-Syn Ha, Sung-Hoo Hong, Ji Youl Lee, Sae Woong Kim   +8 more
doaj   +1 more source

Long-Term Efficacy of Mirabegron Add-On Therapy to Antimuscarinic Agents in Patients With Spinal Cord Injury [PDF]

Annals of Rehabilitation Medicine, 2019
Objective To evaluate the long-term efficacy of mirabegron add-on therapy in patients with spinal cord injury (SCI) based on an urodynamic study.
Seok-Hee Han, In Kyoung Cho, Joo Hwan Jung, Seong Ho Jang, Bum-Suk Lee   +4 more
doaj   +1 more source

The Feasibility and Quality of the European Prescribing Exam: An International Multicenter Pilot Study Among 3109 Medical Students From 16 Medical Schools

Clinical Pharmacology &Therapeutics, EarlyView.
The WHO Global Patient Safety Challenge “Medication Without Harm” emphasizes the need to improve doctors' prescribing competence. Junior doctors are particularly at risk of prescribing errors due to inadequate training. To address this, the European Prescribing Exam was developed to standardize and improve clinical pharmacology and therapeutics (CPT ...
Erik M. Donker, Joost D. Piët, David J. Brinkman, Milan C. Richir, Paraskevi Papaioannidou, Robert Likic, Emilio J. Sanz, Thierry Christiaens, João N. Costa, Fabrizio De Ponti, Ylva Böttiger, Cornelis Kramers, Michiel A. van Agtmael, Jelle Tichelaar, on behalf of the Erasmus+ consortium EuroPE+ and the EACPT Education Working Group, Emilio Sanz, Carla Sans, Ellen van Leeuwen, Haithem Chtioui, Joao Costa, Jitka Rychlickova, Lorena Dima, Romaldas Maciulaitis, Marc Labriffe, Bogdan Tamba, Michiel van Agtmael, Erik Donker   +26 more
wiley   +1 more source

Phenotyping patients with chronic obstructive pulmonary disease and heart failure

ESC Heart Failure, Volume 12, Issue 2, Page 900-911, April 2025.
Central illustration. Abbreviations: ACEi, angiotensin‐converting enzyme inhibitor; ARB, angiotensin receptor blocker; ARNi, angiotensin‐receptor‐neprilysin inhibitor; CI, confidence interval; COPD, chronic obstructive pulmonary disease; CRT, cardiac resynchronization therapy; CV, cardiovascular; EF, ejection fraction; eGFR, estimated glomerular ...
Peter Moritz Becher, Felix Lindberg, Lina Benson, Camilla Hage, Ulf Dahlström, Stephan Rosenkranz, Francesco Cosentino, Giuseppe M.C. Rosano, Stefan Blankenberg, Paulus Kirchhof, Frieder Braunschweig, Lars H. Lund, Gianluigi Savarese   +12 more
wiley   +1 more source