Results 1 to 10 of about 17,562 (163)
Silent agonists for α7 nicotinic acetylcholine receptors
Pharmacological Research, 2023 We discuss models for the activation and desensitization of α7 nicotinic acetylcholine receptors (nAChRs) and the effects of efficacious type II positive allosteric modulators (PAMs) that destabilize α7 desensitized states. Type II PAMs such as PNU-120596 can be used to distinguish inactive compounds from silent agonists, compounds that produce little ...
Roger L. Papke +2 more
openaire +4 more sources
CellsAcetylcholine signaling is attenuated in early Alzheimer’s disease (AD) and other dementias. A significant reduction in the expression of nicotinic acetylcholine receptors (nAChRs) in the brain of AD patients has also been reported in several molecular ...
Eleonora Lacorte +2 more
exaly +3 more sources
eLife, 2022 Nicotinic partial agonists provide an accepted aid for smoking cessation and thus contribute to decreasing tobacco-related disease. Improved drugs constitute a continued area of study. However, there remains no reductionist method to examine the cellular
Aaron L Nichols +18 more
doaj +1 more source
Nicotinic acetylcholine receptor agonists attenuate septic acute kidney injury in mice by suppressing inflammation and proteasome activity. [PDF]
PLoS ONE, 2012 Sepsis is one of the leading causes of acute kidney injury (AKI). Septic patients who develop acute kidney injury (AKI) are at increased risk of death. To date there is no effective treatment for AKI or septic AKI.
Prodyot K Chatterjee +6 more
doaj +1 more source
Acute activation, desensitization and smoldering activation of human acetylcholine receptors. [PDF]
PLoS ONE, 2013 The behavioral effects of nicotine and other nicotinic agonists are mediated by AChRs in the brain. The relative contribution of acute activation versus chronic desensitization of AChRs is unknown. Sustained "smoldering activation" occurs over a range of
Barbara G Campling +2 more
doaj +1 more source
Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators
Molecules, 2023 Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric ...
Dina Manetti +6 more
doaj +1 more source
Ingestion of A Common Plant’s Leaves Leads to Acute Respiratory Arrest and Paralysis: A Case Report
Clinical Practice and Cases in Emergency Medicine, 2020 Background: Nicotiana glauca is a plant known to cause acute toxicity upon ingestion or dermal exposure due to the nicotinic alkaloid, anabasine. Nicotinic alkaloids cause toxicity by acting as agonists on nicotinic-type acetylcholine receptors (nAChRs).
Breelan M. Kear +4 more
doaj +1 more source
Cholinergic anti-inflammatory pathway and COVID-19 [PDF]
BioImpacts, 2022 The cholinergic anti-inflammatory pathway (CAP) first described by Wang et al, 2003 has contemporary interest arising from the COVID-19 pandemic. While tobacco smoking has been considered an aggravating factor in the severity of COVID-19 infections, it ...
Danial Mehranfard, Robert C. Speth
doaj +1 more source
Advances in small molecule selective ligands for heteromeric nicotinic acetylcholine receptors
Pharmacological Research, 2023 The study of nicotinic acetylcholine receptors (nAChRs) has significantly progressed in the last decade, due to a) the improved techniques available for structural studies; b) the identification of ligands interacting at orthosteric and allosteric ...
Carlo Matera +3 more
doaj +1 more source
Medicina, 2015 Objective: The aim of the study was to explore the effect of semi-specific antagonists and agonists of the nicotinic acetylcholine receptors on the paired-pulse facilitation and nicotinic tonic and phasic potentiation of the frog retinotectal synaptic ...
Armuntas Baginskas +2 more
doaj +1 more source