ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience1998
Critical elements determining diversity in agonist binding and desensitization of neuronal nicotinic acetylcholine receptors.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 106 citations in OpenAlex.
- Nicotinic Acetylcholine Receptor Involvement in Inflammatory Bowel Disease and Interactions with Gut Microbiota.International journal of environmental research and public health · 2021Review
- The Constitutive Lack of α7 Nicotinic Receptor Leads to Metabolic Disorders in Mouse.Biomolecules · 2020Article
- Chronic nicotine exposure attenuates the effects of ΔBrain and behavior · 2019Article
- Nicotine and networks: Potential for enhancement of mood and cognition in late-life depression.Neuroscience and biobehavioral reviews · 2018Review
- Insights Into Nicotinic Receptor Signaling in Nicotine Addiction: Implications for Prevention and Treatment.Current neuropharmacology · 2018Review
- The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.The Journal of biological chemistry · 2014Article
- The additional ACh binding site at the α4(+)/α4(-) interface of the (α4β2)2α4 nicotinic ACh receptor contributes to desensitization.British journal of pharmacology · 2013Article
- The energy and work of a ligand-gated ion channel.Journal of molecular biology · 2013Review
- Contribution of α7 nicotinic receptor to airway epithelium dysfunction under nicotine exposure.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Off the beaten path: drug addiction and the pontine laterodorsal tegmentum.ISRN neuroscience · 2013Review
- Action of nicotine and analogs on acetylcholine receptors having mutations of transmitter-binding site residue αG153.The Journal of general physiology · 2013Article
- Levamisole receptors: a second awakening.Trends in parasitology · 2012Review
- Naturally-expressed nicotinic acetylcholine receptor subtypes.Biochemical pharmacology · 2011Review
- Differential contribution of genetic variation in multiple brain nicotinic cholinergic receptors to nicotine dependence: recent progress and emerging open questions.Molecular psychiatry · 2009Review
- Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system.Nature reviews. Drug discovery · 2009Review
- Mammalian nicotinic acetylcholine receptors: from structure to function.Physiological reviews · 2009Review
- Modulation of 5-HT3 receptor desensitization by the light chain of microtubule-associated protein 1B expressed in HEK 293 cells.The Journal of physiology · 2008Article
- Regulation of synaptic transmission and plasticity by neuronal nicotinic acetylcholine receptors.Biochemical pharmacology · 2007Review
- Desensitization of alpha7 nicotinic receptors potentiated the inhibitory effect on M-current induced by stimulation of muscarinic receptors in rat superior cervical ganglion neurons.Journal of neural transmission (Vienna, Austria : 1996) · 2005Article
- A gating mechanism proposed from a simulation of a human alpha7 nicotinic acetylcholine receptor.Proceedings of the National Academy of Sciences of the United States of America · 2005Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
To identify the molecular determinants underlying the pharmacological diversity of neuronal nicotinic acetylcholine receptors, we compared the alpha7 homo-oligomeric and alpha4beta2 hetero-oligomeric receptors. Sets of residues from the regions initially identified within the agonist binding site of the alpha4 subunit were introduced into the alpha7 agonist binding site, carried by the homo-oligomeric alpha7-V201-5HT3 chimera. Introduction of the alpha4 residues 183-191 into alpha7 subunit sequence (chimera C2) selectively increased the apparent affinities for equilibrium binding and for ion channel activation by acetylcholine, resulting in a receptor that no longer displays differences in the responses to acetylcholine and nicotine. Introduction of the alpha4 residues 151-155 (chimera B) produced a approximately 100-fold increase in the apparent affinity for both acetylcholine and nicotine in equilibrium binding measurements. In both cases electrophysiological recordings revealed a much smaller increase (three- to sevenfold) in the apparent affinity for activation, but the concentrations required to desensitize the mutant chimeras parallel the shifts in apparent binding affinity. The data were fitted by a two-state concerted model, and an alteration of the conformational isomerization constant leading to the desensitized state accounts for the chimera B phenotype, whereas alteration of the ligand binding site accounts for the chimera C2 phenotype. Point mutation analysis revealed that several residues in both fragments contribute to the phenotypes, with a critical effect of the G152K and T183N mutations. Transfer of alpha4 amino acids 151-155 and 183-191 into the alpha7-V201-5HT3 chimera thus confers physiological and pharmacological properties typical of the alpha4beta2 receptor.
Indexed as
Identifiers
9425007PMC6792538W1488144458What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.