Results 11 to 20 of about 21,014 (223)

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, Amy E Easton, Yu-Wen Li, Digavalli V Sivarao, Regina Lidge, Kelli M Jones, Debra Post-Munson, Christopher Daly, Nicholas J Lodge, Lizbeth Gallagher, Thaddeus Molski, Richard Pieschl, Ping Chen, Adam Hendricson, Ryan Westphal, James Cook, Christiana Iwuagwu, Daniel Morgan, Yulia Benitex, Dalton King, John E Macor, Robert Zaczek, Richard Olson   +22 more
doaj   +1 more source

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, Hye Jin Kang, Ruogu Gao, Jingjing Wang, Gye Won Han, Jeffrey F. DiBerto, Lijie Wu, Jiahui Tong, Lu Qu, Yiran Wu, Ryan Pileski, Xuemei Li, Xuejun Cai Zhang, Suwen Zhao, Terry Kenakin, Quan Wang, Raymond C. Stevens, Wei Peng, Bryan L. Roth, Zihe Rao, Zhi-Jie Liu   +20 more
doaj   +1 more source

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, Anna Chatzidaki, Daniel Ursu, Emanuele Sher, Neil S Millar   +4 more
doaj   +1 more source

Nicotinic acetylcholine receptors in the synganglion of the tick Ixodes ricinus: Functional characterization using membrane microtransplantation

International Journal for Parasitology: Drugs and Drug Resistance, 2020
Nicotinic acetylcholine receptors are an important class of excitatory receptors in the central nervous system of arthropods. In the ticks Ixodes ricinus, the functional and pharmacological properties of nicotinic receptors located in their neurons are ...
Anaïs Le Mauff, Hamza Chouikh, Alison Cartereau, Claude L. Charvet, Cédric Neveu, Claude Rispe, Olivier Plantard, Emiliane Taillebois, Steeve H. Thany   +8 more
doaj   +1 more source

RNA sequencing data describing transcriptional changes in aorta of ApoE-/- mice after alpha 7 nicotinic acetylcholine receptor (α7nAChR) stimulation

Data in Brief, 2020
This manuscript is a companion paper to Ulleryd M.U. et al., “Stimulation of alpha 7 nicotinic acetylcholine receptor (α7nAChR) inhibits atherosclerosis via immunomodulatory effects on myeloid cells” Atherosclerosis, 2019 [1]. Data shown here include RNA
Marcus A. Ulleryd, Filip Mjörnstedt, Dimitra Panagaki, Li Jin Yang, Kajsa Engevall, Saray Gutierrez, Yixin Wang, Li-Ming Gan, Holger Nilsson, Erik Michaëlsson, Maria E. Johansson   +10 more
doaj   +1 more source

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, Simsek Oguzhan, Yoca Ozge Uysal, Demir Ayse Banu, Tosun Metiner   +4 more
doaj   +1 more source

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
doaj   +1 more source

Activation of muscle nicotinic acetylcholine receptor channels by nicotinic and muscarinic agonists [PDF]

British Journal of Pharmacology, 1999
The dose‐response parameters of recombinant mouse adult neuromuscular acetylcholine receptor channels (nAChR) activated by carbamylcholine, nicotine, muscarine and oxotremorine were measured. Rate constants for agonist association and dissociation, and channel opening and closing, were estimated from single‐channel kinetic analysis.
G, Akk, A, Auerbach
openaire   +2 more sources

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, Fanshawe, TR, Thomas, KH, Theodoulou, A, Hajizadeh, A, Hartman, L, Lindson, N   +6 more
openaire   +4 more sources

Nicotine receptor partial agonists for smoking cessation [PDF]

Cochrane Database of Systematic Reviews, 2016
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).To review the efficacy of nicotine receptor partial agonists, including varenicline and cytisine, for smoking ...
Cahill, Kate, Lindson-Hawley, Nicola, Thomas, Kyla H, Fanshawe, Thomas R, Lancaster, Tim   +4 more
openaire   +16 more sources