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Pharmacophore identification and validation for human nAChR α7 agonists
, 2013 Bo Yu, Liangren Zhang
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Current Drug Targets, 2012
The α7-nAChR plays critical roles in numerous organs and cells by regulating highly organ and cell typespecific functions. In this special issue different Authors have contributed to clarify the different roles played by the α7- nAChR. Post-translational processes such as receptor "underactivation" or "overactivation" are associated in the central ...
Hildegard Shuller +2 more
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The α7-nAChR plays critical roles in numerous organs and cells by regulating highly organ and cell typespecific functions. In this special issue different Authors have contributed to clarify the different roles played by the α7- nAChR. Post-translational processes such as receptor "underactivation" or "overactivation" are associated in the central ...
Hildegard Shuller +2 more
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Neural nAChRs PET imaging probes
Nuclear Medicine Communications, 2014There have been a number of attempts to study PET radioligands for imaging nicotinic acetylcholine receptors (nAChRs) in the human brain, and the most successful tracers found are radioligands for imaging α4β2-nAChRs, which is the main cerebral nAChRs subtype. C-Nicotine and 2-[F]FA have been applied in many studies in humans.
Ye-Xiong Mo, Ya-Fu Yin, Ya-Ming Li
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New-generation radiotracers for nAChR and NET
Nuclear Medicine and Biology, 2005Advances in radiotracer chemistry and instrumentation have merged to make positron emission tomography (PET) a powerful tool in the biomedical sciences. Positron emission tomography has found increased application in the study of drugs affecting the brain and whole body, including the measurement of drug pharmacokinetics (using a positron-emitter ...
Joanna S. Fowler, Yu-Shin Ding
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Journal of Molecular Neuroscience, 1999
In rats, 1 mg/kg twice daily for 10 d of nicotine, a nonselective agonist of nicotinic acetylcholine receptors (nAChRs), fails to change alpha4 and beta2 nAChR subunit mRNA but significantly decreased alpha7 nAChR subunit mRNA and protein expression, which is associated with a 35-40% decrease in the number of 125I-alpha-Bgtx binding sites in ...
James Auta +3 more
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In rats, 1 mg/kg twice daily for 10 d of nicotine, a nonselective agonist of nicotinic acetylcholine receptors (nAChRs), fails to change alpha4 and beta2 nAChR subunit mRNA but significantly decreased alpha7 nAChR subunit mRNA and protein expression, which is associated with a 35-40% decrease in the number of 125I-alpha-Bgtx binding sites in ...
James Auta +3 more
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Myogenin-dependent nAChR clustering in aneural myotubes
Molecular and Cellular Neuroscience, 2006During development of the neuromuscular junction, nerve-derived agrin and the cell substrate laminin stimulate postsynaptic nAChR clustering. This clustering is dependent on activation of the tyrosine kinase, MuSK, which signals receptor clustering via a rapsyn-dependent mechanism.
Daniel Goldman +2 more
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?7 nAChR in Airway Respiratory Epithelial Cells
Current Drug Targets, 2012This review examines the role of α7 nAChR in different types of airway epithelial cells of the normal human bronchial tree. In each of these cells α7 nAChR activation elicits a specific effect. The effect is essentially mitogenic, whereas in the airway basal cells are antiproliferative.
Candida Nastrucci, Patrizia Russo
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Ethanol modulates nicotine-induced upregulation of nAChRs
Brain Research, 2003The use of alcohol and nicotine are highly correlated, suggesting an underlying biochemical interaction. Chronic nicotine exposure results in a deactivation and subsequent upregulation of the expression of nicotinic acetylcholine receptors (nAChRs). Upregulation is thought to represent certain aspects of physical dependence on nicotine. If alcohol also
Douglas P. Dohrman, Cindy K. Reiter
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Journal of Molecular Graphics and Modelling, 2008
Neuronal nicotinic acetylcholine receptors (nAChRs) are important therapeutic targets for various diseases, including Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for cessation of smoking. Based on the recently determined crystal structure of the extracellular domain (ECD) of the mouse nAChR alpha1 subunit complexed with ...
Maria Konstantakaki +4 more
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Neuronal nicotinic acetylcholine receptors (nAChRs) are important therapeutic targets for various diseases, including Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for cessation of smoking. Based on the recently determined crystal structure of the extracellular domain (ECD) of the mouse nAChR alpha1 subunit complexed with ...
Maria Konstantakaki +4 more
openaire +3 more sources