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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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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S5‐01–02: Nicotine and nicotine agonists [PDF]
Alzheimer's & Dementia, 2008 Paul Newhouse
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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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Nicotine receptor partial agonists for smoking cessation [PDF]
Sao Paulo Medical Journal, 2007 Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). Varenicline was developed as a nicotine receptor partial agonist from cytisine, a drug widely used in central
Cahill, Kate +3 more
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Nicotine receptor partial agonists for smoking cessation
Cochrane Database of Systematic Reviews, 2023 Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). This is an update of a Cochrane Review first published in 2007.To assess the effectiveness of nicotine ...
Livingstone-Banks, J +6 more
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Contrasting properties of α7-selective orthosteric and allosteric agonists examined on native nicotinic acetylcholine receptors. [PDF]
PLoS ONE, 2013 Subtype-selective ligands are important tools for the pharmacological characterisation of neurotransmitter receptors. This is particularly the case for nicotinic acetylcholine receptors (nAChRs), given the heterogeneity of their subunit composition.
JasKiran K Gill +4 more
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Effects of kynurenic acid and choline on lipopolysaccharide-induced cyclooxygenase pathway
Türk Biyokimya Dergisi, 2023 Inflammation can be endogenously modulated by the cholinergic anti-inflammatory pathway via calcium (Ca2+)-permeable alpha-7 nicotinic acetylcholine receptor (α7nAChR) ion channel expressed in immune cells.
Baris Elif +4 more
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