Results 181 to 190 of about 31,985 (308)

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

Critical role of the mast cell/tryptase/PAR2 axis in anastrozole‐induced pain

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Anastrozole, an aromatase inhibitor, is used to treat postmenopausal women with hormone receptor‐positive breast cancer, but also induces musculoskeletal pain and can lead to therapeutic regimen suspension. Aromatase inhibitors promote the release of pro‐inflammatory substances from sensitised nerve fibres, which might ...
Maria Fernanda Pessano Fialho, Raquel Tonello, Evelyne Silva Brum, Gabriela Becker, Nigel W. Bunnett, Sara Marchesan Oliveira   +5 more
wiley   +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

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source

Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the D₃ Dopamine Receptor. [PDF]

J Med Chem
Moritz AE, Wang F, Madaras NS, Kelley AM, Snyder KK, Gandhi D, Inbody LR, Akano EO, Shi L, Lane JR, Free RB, Frankowski KJ, Sibley DR.   +12 more
europepmc   +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

ADX106772, an mGlu2 receptor positive allosteric modulator, selectively attenuates oxycodone taking and seeking. [PDF]

Neuropharmacology, 2023
Illenberger JM, Flores-Ramirez FJ, Matzeu A, Lütjens R, Martin-Fardon R.   +4 more
europepmc   +1 more source

The relationship between the cannabinoids and cardiac remodelling: A comprehensive review of pivotal mechanisms and emerging evidence

British Journal of Pharmacology, EarlyView.
Cardiac remodelling and fibrosis after myocardial infarction or during chronic diseases, such as arterial and pulmonary hypertension or diabetes mellitus, continue to be the more important prognostic factors in determining survival, and so the search for effective anti‐fibrotic interventions is an important target for research and therapy in cardiology.
Anna Krzyżewska, Marta Baranowska‐Kuczko, Hanna Kozłowska   +2 more
wiley   +1 more source

Discovery of VU6025733 (AG06827): A Highly Selective, Orally Bioavailable, and Structurally Distinct M₄ Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) with Robust <i>In Vivo</i> Efficacy. [PDF]

ACS Chem Neurosci
Gregro AR, Park C, Long MF, Baker LA, Bollinger KA, Ringuette AE, Peng L, Luscombe VB, Billard NB, Rodriguez AL, Niswender CM, Peng W, Dickerson JW, Rook JM, O'Neill J, Chang S, Boonen HCM, Jensen T, Thomsen MS, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ.   +24 more
europepmc   +1 more source

A homotropic two-state model and auto-antagonism [PDF]

, 2004
Niels Bindslev
core   +1 more source