Results 51 to 60 of about 101,537 (246)

Molecular Mechanisms of Bitopic Ligand Engagement with the M1 Muscarinic Acetylcholine Receptor*

Journal of Biological Chemistry, 2014
Background: Bitopic ligands bind concomitantly to orthosteric and allosteric receptor sites. Results: Residues affecting binding and biased signaling of the selective agonists TBPB and 77-LH-28-1 were identified at the M1 muscarinic receptor. Conclusion:
Peter Keov, Laura Lopez, Shane M. Devine, C. Valant, J. R. Lane, P. Scammells, P. Sexton, A. Christopoulos   +7 more
semanticscholar   +1 more source

Endothelium‐Independent Relaxation of Alkaloid Boldine in Isolated Aortas From Normotensive and Hypertensive Rats: Participation of Ca2+ Channels

Chemistry &Biodiversity, EarlyView.
Involvement of Ca2+ channels in boldine‐induced vascular relaxation. ABSTRACT The regulation of vascular tone plays a fundamental role in blood pressure homeostasis and still represents a significant challenge in clinical practice. Boldine, a naturally occurring alkaloid from Peumus boldus, has emerged as a compound of interest due to its therapeutic ...
Martina Odebrecht Cavichiolo, Rita de Cássia Vilhena da Silva, Valdir Cechinel Filho, Priscila de Souza   +3 more
wiley   +1 more source

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of 18F‐Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3

ChemMedChem, EarlyView.
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Miguel A. Herrera‐Rueda, Maxwell A. Boateng, Melinda Wuest, Frederick G. West, Frank Wuest   +4 more
wiley   +1 more source

Structure and Dynamics of the M3 Muscarinic Acetylcholine Receptor

Nature, 2012
Acetylcholine, the first neurotransmitter to be identified, exerts many of its physiological actions via activation of a family of G-protein-coupled receptors (GPCRs) known as muscarinic acetylcholine receptors (mAChRs). Although the five mAChR subtypes (
A. Kruse, Jianxin Hu, Albert C. Pan, Daniel H Arlow, D. Rosenbaum, Erica Rosemond, Hillary F. Green, Tong Liu, P. S. Chae, R. Dror, D. Shaw, W. Weis, J. Wess, B. Kobilka   +13 more
semanticscholar   +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

Neurodevelopmental features in KCNQ2 developmental and epileptic encephalopathy may have limited associations with KV7.2 dysfunction

Epilepsia Open, EarlyView.
Abstract Objective Variants in KCNQ2 encoding the voltage‐gated potassium channel KV7.2 are associated with developmental and epileptic encephalopathy (DEE) of varying severity. This study examined the relationship of KCNQ2 variant dysfunction with the neurodevelopmental phenotype of individuals with KCNQ2‐DEE. Methods A parent‐reported survey gathered
Jessa S. Bidwell, Carlos G. Vanoye, Reshma R. Desai, Anne T. Berg, Alfred L. George Jr   +4 more
wiley   +1 more source

Perturbed synaptic adhesion molecules signaling in neurodevelopmental disorders: The impact of metal neurotoxicity

Ibrain, EarlyView.
Synaptic adhesion molecules (SAM) are essential for the formation, maturation, function, plasticity, and assembly of synaptic connections, all critical for normal neurodevelopment. Excessive exposure to neurotoxic metals during development could disrupt the developing brain and potentially lead to neurodevelopmental disorders (NDDs).
Toheeb O. Oyerinde, Victor E. Anadu, Tobiloba S. Olajide, Ileje I. Ukwubile, Olayemi K. Ijomone, Kingsley A. Iteire, Michael Aschner, Omamuyovwi M. Ijomone   +7 more
wiley   +1 more source

Gαq-Coupled Muscarinic Acetylcholine Receptors Enhance Nicotinic Acetylcholine Receptor Signaling in Caenorhabditis elegans Mating Behavior

Journal of Neuroscience, 2007
In this study, we address why metabotropic and ionotropic cholinergic signaling pathways are used to facilitate motor behaviors. We demonstrate that a Gαq-coupled muscarinic acetylcholine receptor (mAChR) signaling pathway enhances nicotinic ...
Yishi Liu, B. LeBoeuf, L. R. Garcia
semanticscholar   +1 more source

Molecular Biological Mechanisms of Yuan Zhi Powder in the Treatment of Alzheimer’s Disease: an Analysis Based on Network Pharmacology

Digital Chinese Medicine, 2018
: Objective To predict the main active ingredients, potential targets and molecular mechanisms of Yuan Zhi powder in treatment of dementia by using network pharmacology.Methods A database of chemical constituents of Yuan Zhi powder was constructed by ...
Wei-Jie Qiang, Ying Chen, Fu-Yuan He, Mei-Feng Xiao, Wei-Yan Cai, Yi-Fei Dai, Qing Yang, Yu-Jie Li, Xiao-Gang Weng, Qi Li, Ya-Jie Wang, Xiao-Xin Zhu   +11 more
doaj   +1 more source

Wuda Granule Improves the Gastrointestinal Motility via Gut‐Brain Axis in Beagle Dogs

iMetaMed, EarlyView.
Stress sensors were implanted in the gastric body, sinus, duodenum, jejunum, and colon of beagle dogs to record gastrointestinal motility. Gastrointestinal contractile motility was assessed before and after the lateral ventricular injection of Wuda granule, intravenous atropine instillation, and bilateral cervical vagotomy.
Zhi Jiang, Xing Li, Qicheng Chen, Zhiqiang Chen, Lixing Cao, Hailin Tang   +5 more
wiley   +1 more source