Nicotinic acetylcholine receptor agonist attenuates ILC2-dependent airway hyperreactivity
Airway hyperreactivity is driven by type 2 cytokines produced by ILC2 and Th2 cells. Here the authors show that an α7-nicotinic receptor agonist (GTS-21) inhibits ILC2 responses and is therapeutic against Alternaria-induced airway hyperreactivity in a ...
Lauriane Galle-Treger+7 more
doaj +2 more sources
TC299423, a Novel Agonist for Nicotinic Acetylcholine Receptors [PDF]
(E)-5-(Pyrimidin-5-yl)-1,2,3,4,7,8-hexahydroazocine (TC299423) is a novel agonist for nicotinic acetylcholine receptors (nAChRs). We examined its efficacy, affinity, and potency for α6β2∗ (α6β2-containing), α4β2∗, and α3β4∗ nAChRs, using [125I ...
Teagan R. Wall+12 more
doaj +5 more sources
Nicotinic Agonist Inhibits Cardiomyocyte Apoptosis in CVB3-Induced Myocarditis via α3β4-nAChR/PI3K/Akt-Dependent Survivin Upregulation [PDF]
Background Cardiomyocyte apoptosis is critical for the development of coxsackievirus B3- (CVB3-) induced myocarditis, which is a common cardiac disease that may result in heart failure or even sudden death.
Pi-Hong Li+9 more
semanticscholar +2 more sources
The Nicotinic Agonist Cytisine: The Role of the NH···N Interaction [PDF]
We report a detailed structural study of cytisine, an alkaloid used to help with smoking cessation, looking forward to unveiling its role as a nicotinic agonist. High-resolution rotational spectroscopy has allowed us to characterize two different conformers exhibiting axial and equatorial arrangements of the piperidinic NH group.
Raúl Aguado+5 more
openaire +4 more sources
Innate Immunity and Inflammation Post-Stroke: An α7-Nicotinic Agonist Perspective [PDF]
Stroke is one of the leading causes of death and long-term disability, with limited treatment options available. Inflammation contributes to damage tissue in the central nervous system across a broad range of neuropathologies, including Alzheimer’s ...
Silke Neumann+4 more
semanticscholar +2 more sources
Effect of subchronically administered GTS-21 [3-(2,4-dimethoxybenzylidene)-anabaseine dihydrochloride], a selective nicotinic agonist, on neuronal cell loss caused by nucleus basalis magnocellularis (nBM) lesion was studied in rats.
Masato Nanri+4 more
openalex +2 more sources
UB-165: A Novel Nicotinic Agonist with Subtype Selectivity Implicates the α4β2* Subtype in the Modulation of Dopamine Release from Rat Striatal Synaptosomes [PDF]
Presynaptic nicotinic acetylcholine receptors (nAChRs) on striatal synaptosomes stimulate dopamine release. Partial inhibition by the α3β2-selective α-conotoxin-MII indicates heterogeneity of presynaptic nAChRs on dopamine terminals.
Christopher G. V. Sharples+10 more
openalex +2 more sources
α7 Nicotinic Agonist AR-R17779 Protects Mice against 2,4,6-Trinitrobenzene Sulfonic Acid-Induced Colitis in a Spleen-Dependent Way [PDF]
The existence of a cholinergic anti-inflammatory pathway negatively modulating the inflammatory and immune responses in various clinical conditions and experimental models has long been postulated.
Andrea Grandi+7 more
doaj +2 more sources
Agonist efficiency links binding and gating in a nicotinic receptor
Receptors signal by switching between resting (C) and active (O) shapes (‘gating’) under the influence of agonists. The receptor’s maximum response depends on the difference in agonist binding energy, O minus C.
Dinesh C Indurthi, Anthony Auerbach
doaj +3 more sources
Antinociceptive property of the nicotinic agonist AG‐4 in rodents [PDF]
AG-4 has been characterized as a nicotinic agonist by binding (K i = 26 ± 1.4 μM) and in vitro functional assays. The antinociceptive effect of AG-4 was examined in mice and rats, using the hot plate, abdominal constriction, and paw-pressure tests.
C. Ghelardini+6 more
semanticscholar +5 more sources