The Nicotinic Agonist Cytisine: The Role of the NH···N Interaction. [PDF]
J Phys Chem Lett, 2022 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.
Aguado R +5 more
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TC299423, a Novel Agonist for Nicotinic Acetylcholine Receptors [PDF]
Frontiers in Pharmacology, 2017 (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
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α7 Nicotinic Agonist AR-R17779 Protects Mice against 2,4,6-Trinitrobenzene Sulfonic Acid-Induced Colitis in a Spleen-Dependent Way [PDF]
Frontiers in Pharmacology, 2017 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
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Agonist efficiency links binding and gating in a nicotinic receptor
eLife, 2023 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
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Conformational dynamics of a nicotinic receptor neurotransmitter site [PDF]
eLifeAgonists enhance receptor activity by providing net-favorable binding energy to active over resting conformations, with efficiency (η) linking binding energy to gating.
Mrityunjay Singh +4 more
doaj +2 more sources
S5‐01–02: Nicotine and nicotine agonists [PDF]
Alzheimer's & Dementia, 2008 Paul Newhouse
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Pilot safety evaluation of varenicline for the treatment of methamphetamine dependence [PDF]
Journal of Experimental Pharmacology, 2009 Todd Zorick1, Rajkumar J Sevak1, Karen Miotto1, Steven Shoptaw2,4, Aimee-Noelle Swanson2, Clayton Clement1, Richard De La Garza II1*, Thomas F Newton1*, Edythe D London1,3,41Departments of Psychiatry and Biobehavioral Sciences, 2Family Medicine ...
Todd Zorick +3 more
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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
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The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia. [PDF]
PLoS ONE, 2016 The development of alpha7 nicotinic acetylcholine receptor agonists is considered a promising approach for the treatment of cognitive symptoms in schizophrenia patients. In the present studies we characterized the novel agent, (2R)-N-(6-(1H-imidazol-1-yl)
Linda J Bristow +22 more
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Structural insights into the human niacin receptor HCA2-Gi signalling complex
Nature Communications, 2023 Hydroxyl-carboxylic acid receptor 2 (HCA2) functions as a high-affinity receptor for nicotinic acid (vitamin B3). Here, authors report the cryo-EM structure of the HCA2-Gi complex with the agonist MK-6892 and inactive state crystal structures of mutation
Yang Yang +20 more
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