Results 201 to 210 of about 81,932 (256)

Is there a role for cannabidiol in obesity, metabolic syndrome and binge eating?

British Journal of Pharmacology, EarlyView.
Cannabidiol (CBD) is one of the most abundant phytocannabinoids isolated from the Cannabis sativa plant. CBD is a lipophilic, non‐intoxicating substance that differently from Δ9‐tetrahydrocannabinol (Δ9‐THC) does not present the typical profile of a drug of abuse.
Luca Botticelli, Emanuela Micioni Di Bonaventura, Giacomo Einaudi, Gustavo Provensi, Alessia Costa, Claudio D'Addario, Carlo Cifani, Maria Vittoria Micioni Di Bonaventura   +7 more
wiley   +1 more source

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

British Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source

Novel approaches for drug development against chronic primary pain: A systematic review

British Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus, Éva Borbély, Andreas Goebel, Ralf Baron, Zsófia Hajna, Zsuzsanna Helyes   +5 more
wiley   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Variable electrophysiology before and after block of the two delayed rectifier potassium channels in groups of isolated rabbit ventricular cells

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Between‐cell differences in ventricular cardiomyocyte action potential duration (APD) and responses to ion channel block may contribute to pro‐arrhythmic dispersion of myocardial repolarisation. This study quantifies between‐cell physiological and pharmacological variability in the rabbit left ventricle (LV) and uses ...
Rebecca J. Gilchrist, Muhamad Hifzhudin Noor Aziz, Francis L. Burton, Radostin D. Simitev, Rachel C. Myles, Godfrey L. Smith   +5 more
wiley   +1 more source

Cancer pain: current practice and emerging targets

British Journal of Pharmacology, EarlyView.
Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye, Marcin Chwistek, Zhiting Gong, Vanessa Uzonwanne, Xiaojie Shi, Arpad Szallasi   +5 more
wiley   +1 more source

Defining AV2‐1 as a novel pharmacological probe to target human and rodent TRPV2

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Transient receptor potential vanilloid 2 (TRPV2) is a non‐selective cation channel implicated in immune cell functions. However, progress in understanding TRPV2 has been limited by a lack of potent and selective pharmacological tools, particularly those targeting the human variant. We aimed to identify and characterise a
Andrea Leipe, Julia A. Rocereta, Ruth A. Pumroy, Andreas Leffler, Michael Schaefer, Vera Moiseenkova‐Bell, Kerstin Hill   +6 more
wiley   +1 more source

Pharmacological treatment with a GABA(A) receptor modulator and a selective serotonin reuptake inhibitor as a mitigation strategy against aircraft noise‐induced cardiovascular and neuronal damage

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Noise pollution, particularly by aircraft, is a significant risk factor for cardiovascular disease. Aircraft noise activates stress response pathways in the brain, via the amygdala, the sympathetic nervous system and the hypothalamic–pituitary–adrenal axis.
Ivana Kuntić, Marin Kuntić, Jiayin Zheng, Leonardo Nardi, Matthias Oelze, Arijan Valar, Dominika Mihaliková, Lea Strohm, Hans‐Georg Buchholz, Nicole Bausbacher, Simon Lange, Henning Ubbens, Qi Tang, Liyu Zhang, Guilherme Horta, Paul Stamm, Omar Hahad, Axel Methner, Sebastian Steven, Huige Li, Mathias Schreckenberger, Dilja Krueger‐Burg, Adrian Gericke, Michael J. Schmeisser, Thomas Münzel, Andreas Daiber   +25 more
wiley   +1 more source