Results 101 to 110 of about 37,595 (283)

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

The peroxisome proliferator activated receptor gamma agonist pioglitazone increases functional expression of the glutamate transporter excitatory amino acid transporter 2 (EAAT2) in human glioblastoma cells

, 2015
Jared Ching, Stephanie Amiridis, Stanley S. Stylli, Andrew R. Bjorksten, Nicole Kountouri, Thomas Zheng, Lucy Paradiso, Rodney B. Luwor, Andrew Morokoff, Terence J. O’Brien, Andrew H. Kaye   +10 more
openalex   +2 more sources

Evaluation of preclinical antipsychotic models used to support first‐in‐human clinical trials

British Journal of Pharmacology, EarlyView.
Abstract Schizophrenia is regarded as a complex and heterogeneous psychiatric disorder, characterised by diverse symptoms and comorbidities, which complicate both clinical management and drug development. Current pharmacological treatment, primarily based on dopamine D2 receptor antagonism or partial agonism, which has not markedly progressed since the
Thi Viet Ha Nguyen, Declan P. McKernan, John P. Kelly   +2 more
wiley   +1 more source

Protectin D1 and maresin 1 attenuate airway hyperreactivity induced by IL‐13 in human isolated small bronchi

British Journal of Pharmacology, EarlyView.
Background and Purpose Interleukin (IL)‐13 is implicated in airway hyperreactivity (AHR), a key feature of asthma. We explored the potential anti‐AHR activity of selected specialised pro‐resolving mediators (SPMs) in IL‐13‐induced AHR models, using human bronchial smooth muscle cells (BSMCs) and human isolated bronchi.
Willem Abma, Sven‐Erik Dahlén, Craig E. Wheelock, Mikael Adner, Mamdoh Al‐Amerie, Erik Sachs, Kasra Vali Jalali, Leonardo De Maria, Henric Olsson, Jesper Säfholm   +9 more
wiley   +1 more source

Effects on Breathing of Agonists to μ-opioid or GABA\u3csub\u3eA\u3c/sub\u3e Receptors Dialyzed into the Ventral Respiratory Column of Awake and Sleeping Goats [PDF]

, 2017
Pulmonary ventilation (V̇I) in awake and sleeping goats does not change when antagonists to several excitatory G protein-coupled receptors are dialyzed unilaterally into the ventral respiratory column (VRC).
Burgraff, Nicholas J., Crumley, Emma, Forster, Hubert V., Hodges, Matthew R., Langer, Thomas M., III, Neumueller, Suzanne E., Pan, Lawrence, Talwar, Sawan   +7 more
core   +1 more source

A PK/PD study on antihyperalgesia by an α2/3‐GABAA receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose GABAA receptors (GABAARs) are heteropentameric ion channels that control almost all CNS functions, including spinal nociception. Most GABAARs contain a γ2 subunit but differ in their α and β subunit composition. TPA023B is an α2/α3 subtype selective, non‐sedative, positive allosteric modulator (PAM) with antihyperalgesic
Elena Neumann, Mariana O. Popa, Karen T. Elvers, Misa Oyama, Daniel Ulrich, Marcus Hanley, Gui Jie Feng, Thomas Hathaway, William T. Ralvenius, Thomas Grampp, Dietmar Benke, John R. Atack, Hanns Ulrich Zeilhofer   +12 more
wiley   +1 more source

Loss of Glial Glutamate and Aspartate Transporter (Excitatory Amino Acid Transporter 1) Causes Locomotor Hyperactivity and Exaggerated Responses to Psychotomimetics: Rescue by Haloperidol and Metabotropic Glutamate 2/3 Agonist

, 2008
Rose‐Marie Karlsson, Kohichi Tanaka, Markus Heilig, Andrew Holmes   +3 more
openalex   +2 more sources

Blunted Cystine–Glutamate Antiporter Function in the Nucleus Accumbens Promotes Cocaine-induced Drug Seeking [PDF]

, 2008
Repeated cocaine alters glutamate neurotransmission, in part, by reducing cystine–glutamate exchange via system xc−, which maintains glutamate levels and receptor stimulation in the extrasynaptic compartment.
Abdulhameed, Omer, Baker, David A., Grier, Mark D., Kau, Kristen S., Madayag, Aric, Mantsch, John R.   +5 more
core   +1 more source

Feedback control of excitability and high K+ induced epileptiform bursts in male rat hippocampal slices with a photocaged adenosine A1 receptor agonist

British Journal of Pharmacology, EarlyView.
Background and Purpose Adenosine is a potent regulator of neurotransmission and neuronal excitability, through activation of Gi coupled adenosine A1 receptors (A1Rs). Adenosine has gained interest as an anticonvulsant because of its endogenous involvement in ending seizure activity, but peripheral side effects require local application.
Erine Craey, Marijke Vergaelen, Serge Van Calenbergh, Jeroen Spanoghe, Evelien Carrette, Kristl Vonck, Paul Boon, Wytse J. Wadman, Robrecht Raedt   +8 more
wiley   +1 more source