Results 101 to 110 of about 50,615 (267)

Therapeutic potential of small molecules that block receptor‐induced Kv7/M‐current suppression in neuroprotection, seizures, and pain

British Journal of Pharmacology, EarlyView.
Receptor‐induced Kv7/M‐current suppression increases neuronal activity and contributes to pathology of several conditions. A new class of Kv7 modulators identified in this study attenuates M‐current suppression and shows therapeutic effects. Abstract Background and Purpose Neuronal Kv7 channels generate low voltage–gated potassium currents known as the
Young Woo Kim, Pavan Kumar Behara, Lamees Alhassen, Cindy Wong, Olivier Civelli, Naoto Hoshi   +5 more
wiley   +1 more source

Drugs that act on both G protein‐coupled receptors (GPCRs) and kinases: potentiation of effects, side effects and general aspects of drug pleiotropy

British Journal of Pharmacology, EarlyView.
Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren, Aleksandr Sokolov, Flavio Ballante, Robert Fredriksson, Francisco Lagunas‐Rangel, Alexander S. Hauser, Stefan Knapp, Jörgen Jonsson, Helgi B. Schiöth   +8 more
wiley   +1 more source

Pilocarpine induces the residual secretion of salivary fluid in perfused submandibular glands of rats.

PLoS ONE, 2019
Pilocarpine is an M3 muscarinic agonist that is widely used for the treatment of xerostomia caused by various diseases and medical conditions. Pilocarpine induced the secretion of salivary fluid in perfused submandibular glands of rats.
Takanori Narita, Bing Qi, Masataka Murakami, Hiroshi Sugiya   +3 more
doaj   +1 more source

Altered brainstem responses to modafinil in schizophrenia: implications for adjunctive treatment of cognition. [PDF]

, 2018
Candidate pro-cognitive drugs for schizophrenia targeting several neurochemical systems have consistently failed to demonstrate robust efficacy. It remains untested whether concurrent antipsychotic medications exert pharmacodynamic interactions that ...
Carter, Cameron S, Minzenberg, Michael J, Soosman, Steffan K, Yoon, Jong H   +3 more
core   +3 more sources

ADAM17 and its proteolytic targets in disease pathogenesis

The FEBS Journal, EarlyView.
ADAM17 as a multifunctional sheddase with contrasting roles across inflammatory, metabolic, cardiovascular, and neoplastic diseases. Through regulated activation by iRhom, iTAP/FRMD8, and tetraspanins, ADAM17 cleaves diverse membrane ligands and receptors, thereby promoting inflammation, fibrosis, obesity, insulin resistance, and tumor progression ...
Abdulbasit Amin, Marina Badenes
wiley   +1 more source

Forced Expiratory Flow (FEF25–75%) as a Clinical Endpoint in Children and Adolescents with Symptomatic Asthma Receiving Tiotropium: A Post Hoc Analysis

Pulmonary Therapy, 2020
Introduction In pediatric patients with asthma, measurements of forced expiratory volume in 1 s (FEV1) may be normal or may not correlate with symptom severity.
Stanley J. Szefler, Stanley Goldstein, Christian Vogelberg, George W. Bensch, John Given, Branko Jugovic, Michael Engel, Petra M. Moroni-Zentgraf, Ralf Sigmund, Eckard H. Hamelmann   +9 more
doaj   +1 more source

Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]

, 2007
Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung, Li, Bo, Scarselli, Marco, Wess, Jürgen   +3 more
core   +1 more source

Evolving treatments for Sjögren disease: current approaches and emerging targets

Internal Medicine Journal, EarlyView.
Abstract Sjögren disease (SjD) is a prevalent systemic autoimmune condition characterised by exocrine gland dysfunction, systemic inflammation and heterogeneous organ involvement. Current management remains largely symptomatic, with no approved disease‐modifying therapies available and substantial unmet clinical need. However, advances in understanding
Mansi Bhurani, Adrian Y. S. Lee, Maureen Rischmueller, Alberta Hoi   +3 more
wiley   +1 more source

Anticholinergic Medication Burden Scales: A Systematic Review

Journal of the American Geriatrics Society, EarlyView.
ABSTRACT Background Anticholinergic burden refers to the cumulative anticholinergic effect of all medications taken by an individual. Anticholinergic burden scales help identify patients at risk of anticholinergic adverse effects and guide prescribing. However, substantial variation exists between scales, with no gold standard identified.
Orla Vennard, Carrie Stewart, Mansi Tolia, Roy L. Soiza, Phyo K. Myint   +4 more
wiley   +1 more source

Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]

, 2009
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros, Cho, D. A. Dougherty, Dougherty, Dougherty, Dougherty, Doupnik, Gallivan, H. A. Lester, Hibert, Hopkins, Huang, Huang, K. S. Bower, Klabunde, Kofuji, Krapivinsky, Lagerstrom, Lu, Lu, M. M. Torrice, Ma, Mark, Nemeth, Nowak, Palczewski, Rasmussen, Schwartz, Warne, Xiu, Zacharias, Zhong   +31 more
core   +3 more sources