Results 71 to 80 of about 15,706 (256)
Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias
Frontiers in Pharmacology, 2021 The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen +7 more
doaj +1 more source
Novel aspects of cholinergic regulation of colonic ion transport [PDF]
, 2015 Nicotinic receptors are not only expressed by excitable tissues, but have been identified in various epithelia. One aim of this study was to investigate the expression of nicotinic receptors and their involvement in the regulation of ion transport across
Bader, Sandra, Diener, Martin
core +1 more source
Status epilepticus: Updates on mechanisms and treatments
Epilepsia Open, EarlyView.Abstract Status epilepticus (SE) consists of prolonged, self‐sustaining seizures and is a common neurological emergency that causes respiratory compromise and neuronal injury. Without prompt treatment, the seizures can become resistant to benzodiazepines, leading to the progressive evolution of established, refractory, and super‐refractory SE.
Suchitra Joshi, Jaideep Kapur
wiley +1 more source
New strategic insights into managing fungal biofilms [PDF]
, 2015 Fungal infections have dramatically increased in the last decades in parallel with an increase of populations with impaired immunity, resulting from medical conditions such as cancer, transplantation or other chronic diseases.
Borghi, Elisa +6 more
core +4 more sources
Spirocyclic Diamine Scaffolds for Medicinal Chemistry
Helvetica Chimica Acta, EarlyView.Here we enumerated 391 spirocyclic diamine drug scaffolds with ring sizes four to eight and found that most of them are unknown. We prepared four novel such spirocycles and discovered a micromolar inhibitor of the M4 muscarinic receptor. ABSTRACT Medicinal chemistry requires the exploration of structurally diverse compound families to expand the ...
Aline Carrel +3 more
wiley +1 more source
Molecular Mechanisms of Bitopic Ligand Engagement with the M1 Muscarinic Acetylcholine Receptor [PDF]
Journal of Biological Chemistry, 2014 TBPB and 77-LH-28-1 are selective agonists of the M1 muscarinic acetylcholine receptor (mAChR) that may gain their selectivity through a bitopic mechanism, interacting concomitantly with the orthosteric site and part of an allosteric site. The current study combined site-directed mutagenesis, analytical pharmacology,and molecular modeling to gain ...
Peter, Keov +7 more
openaire +2 more sources
Pharmacological evaluation of the long-term effects of xanomeline on the M(1) muscarinic acetylcholine receptor. [PDF]
PLoS ONE, 2010 Xanomeline is a unique agonist of muscarinic receptors that possesses functional selectivity at the M(1) and M(4) receptor subtypes. It also exhibits wash-resistant binding to and activation of the receptor.
Marianne K O Grant +5 more
doaj +1 more source
Acta Psychiatrica Scandinavica, EarlyView.ABSTRACT Background Schizophrenia is characterized by positive, negative, and cognitive symptoms. Current pharmacological treatments often fail to address cognitive deficits. In this review of clinical trials, we aim to identify studies that explore neurobiological (non‐psychological) strategies to address Cognitive Impairment Associated with ...
Bahareh Peyrovian +3 more
wiley +1 more source
Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes [PDF]
Science, 2019 Choosing a partner G protein–coupled receptors (GPCRs) bind ligands outside the cell and trigger events inside the cell by selectively binding and activating specific G proteins. The selectivity occurs even among highly related GPCRs.
Shoji Maeda +4 more
openaire +2 more sources
Forebrain Cholinergic Signaling Regulates Innate Immune Responses and Inflammation
Frontiers in Immunology, 2019 The brain regulates physiological functions integral to survival. However, the insight into brain neuronal regulation of peripheral immune function and the neuromediator systems and pathways involved remains limited. Here, utilizing selective genetic and
Kurt R. Lehner +32 more
doaj +1 more source