Investigation of the Molecular Mechanism of the α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator PNU-120596 Provides Evidence for Two Distinct Desensitized States

No abstract is available for this paper.

• Publication year

  2011

• Venue

  Molecular Pharmacology

• Publication date

  2011-12-01

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1124/mol.111.074302PMID 21885620PMCID PMC3228536
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Calcium signalling mediated through α7 and non‐α7 nAChR stimulation is differentially regulated in bovine chromaffin cells to induce catecholamine release

  2011influential reference
• Characterization of 2-[[4-Fluoro-3-(trifluoromethyl)phenyl]amino]-4-(4-pyridinyl)-5-thiazolemethanol (JNJ-1930942), a Novel Positive Allosteric Modulator of the α7 Nicotinic Acetylcholine Receptor

  2011cited by this paper
• The effective opening of nicotinic acetylcholine receptors with single agonist binding sites

  2011cited by this paper
• Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.

  2011cited by this paper
• Functional Characterization and High-Throughput Screening of Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors in IMR-32 Neuroblastoma Cells

  2011cited by this paper
• Working with OpusXpress: methods for high volume oocyte experiments.

  2010cited by this paper
• Tethered Agonist Analogs as Site-Specific Probes for Domains of the Human α7 Nicotinic Acetylcholine Receptor that Differentially Regulate Activation and Desensitization

  2010cited by this paper
• Positive allosteric modulation of alpha7 neuronal nicotinic acetylcholine receptors: lack of cytotoxicity in PC12 cells and rat primary cortical neurons.

  2009cited by this paper
• Activation and Desensitization of Nicotinic α7-type Acetylcholine Receptors by Benzylidene Anabaseines and Nicotine

  2009cited by this paper
• Tricks of Perspective: Insights and Limitations to the Study of Macroscopic Currents for the Analysis of nAChR Activation and Desensitization

  2009cited by this paper
• In Vitro Pharmacological Characterization of a Novel Allosteric Modulator of α7 Neuronal Acetylcholine Receptor, 4-(5-(4-Chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), Exhibiting Unique Pharmacological Profile

  2009cited by this paper
• Old and New Pharmacology: Positive Allosteric Modulation of the α7 Nicotinic Acetylcholine Receptor by the 5-Hydroxytryptamine2B/C Receptor Antagonist SB-206553 (3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b′]di pyrrole-1(2H)-carboxamide)

  2009cited by this paper
• Editorial: To channel or not to channel? Functioning of nicotinic acetylcholine receptors in leukocytes

  2009cited by this paper
• Diversity of vertebrate nicotinic acetylcholine receptors.

  2009cited by this paper
• Structural determinants for interaction of partial agonists with acetylcholine binding protein and neuronal α7 nicotinic acetylcholine receptor

  2009cited by this paper
• The Interface between Extracellular and Transmembrane Domains of Homomeric Cys-Loop Receptors Governs Open-Channel Lifetime and Rate of Desensitization

  2008cited by this paper
• Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras.

  2008cited by this paper
• Potentiation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site

  2008cited by this paper
• Agonist activation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site

  2008cited by this paper
• On the nature of partial agonism in the nicotinic receptor superfamily

  2008cited by this paper
• Distinct Profiles of α7 nAChR Positive Allosteric Modulation Revealed by Structurally Diverse Chemotypes

  2007cited by this paper
• Reversal of Agonist Selectivity by Mutations of Conserved Amino Acids in the Binding Site of Nicotinic Acetylcholine Receptors*

  2007cited by this paper
• Nootropic α7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators

  2007cited by this paper
• An α7 Nicotinic Acetylcholine Receptor Gain-of-Function Mutant That Retains Pharmacological Fidelity

  2005influential reference
• A Novel Positive Allosteric Modulator of the α7 Neuronal Nicotinic Acetylcholine Receptor: In Vitro and In Vivo Characterization

  2005cited by this paper
• Restoration of single-channel currents using the segmental k-means method based on hidden Markov modeling.

  2004cited by this paper
• Molecular dissection of tropisetron , an 7 nicotinic acetylcholine receptor-selective partial agonist

  2004cited by this paper
• Human α4β2 Acetylcholine Receptors Formed from Linked Subunits

  2003cited by this paper
• Human alpha4beta2 acetylcholine receptors formed from linked subunits.

  2003cited by this paper
• The C.elegans ric‐3 gene is required for maturation of nicotinic acetylcholine receptors

  2002cited by this paper
• Comparative pharmacology of rat and human α7 nAChR conducted with net charge analysis

  2002cited by this paper
• Choline and acetylcholine have similar kinetic properties of activation and desensitization on the alpha7 nicotinic receptors in rat hippocampal neurons.

  2000cited by this paper
• α7 Receptor-selective agonists and modes of α7 receptor activation

  2000cited by this paper
• alpha7 receptor-selective agonists and modes of alpha7 receptor activation.

  2000cited by this paper
• Expression and channel properties of alpha-bungarotoxin-sensitive acetylcholine receptors on chick ciliary and choroid neurons.

  2000cited by this paper
• Characterization of the neuroprotective and toxic effects of alpha7 nicotinic receptor activation in PC12 cells.

  1999cited by this paper
• Characterization of the neuroprotective and toxic effects of α7 nicotinic receptor activation in PC12 cells

  1999cited by this paper
• The correction of alpha7 nicotinic acetylcholine receptor concentration-response relationships in Xenopus oocytes.

  1998cited by this paper
• Paradoxical allosteric effects of competitive inhibitors on neuronal α7 nicotinic receptor mutants

  1997cited by this paper
• Neuronal nicotinic alpha 7 receptor expressed in Xenopus oocytes presents five putative binding sites for methyllycaconitine.

  1996cited by this paper
• Inhibition of nicotinic acetylcholine receptors by bis (2,2,6,6-tetramethyl- 4-piperidinyl) sebacate (Tinuvin 770), an additive to medical plastics.

  1994cited by this paper
• Fast events in single‐channel currents activated by acetylcholine and its analogues at the frog muscle end‐plate.

  1985cited by this paper
• Fitting and Statistical Analysis of Single-Channel Records

  1983cited by this paper
• Structural and functional properties of the acetylcholine receptor protein in its purified and membrane-bound states.

  1978cited by this paper
• Nicotinic acetylcholine receptors.

  1977cited by this paper
• An Effective Opening.

  1969influential reference

• Structural basis for allosteric agonism of human α7 nicotinic acetylcholine receptors

  2025cites this paper
• Inhibition of levodopa-induced abnormal involuntary movements (AIMs) using a selective α7 nicotinic positive allosteric modulator.

  2025cites this paper
• Hidden complexity of α7 nicotinic acetylcholine receptor desensitization revealed by MD simulations and Markov state modeling

  2025influential citation
• Enantiospecific Positive Allosteric Modulation of α4β2 Nicotinic Receptor Subtypes.

  2025cites this paper
• Exposing the latent phenotype of Gulf War Illness: examination of the mechanistic mediators of cognitive dysfunction

  2024cites this paper
• Potential impacts of titanium dioxide nanoparticles on the biochemical and behavioural status of the amphipods Talitrus saltator (Amphipoda, Talitridae)

  2024cites this paper
• The many enigmas of nicotine.

  2024cites this paper
• Structural mechanisms of α7 nicotinic receptor allosteric modulation and activation.

  2024cites this paper
• Symmetrical Bispyridinium Compounds Act as Open Channel Blockers of Cation-Selective Ion Channels

  2024cites this paper
• New Alpha9 nAChR Ligands Based on a 5-(Quinuclidin-3-ylmethyl)-1,2,4-oxadiazole Scaffold.

  2024cites this paper
• Neuroprotective amyloid β N‐terminal peptides differentially alter human α7‐ and α7β2‐nicotinic acetylcholine (nACh) receptor single‐channel properties

  2024cites this paper
• Pharmacological profiles and anti-inflammatory activity of pCN-diEPP and mCN-diEPP, new alpha9alpha10 nicotinic receptor ligands.

  2023cites this paper
• Deepening the understanding of CNVs on chromosome 15q11–13 by using hiPSCs: An overview

  2023influential citation
• Silent agonists for α7 nicotinic acetylcholine receptors.

  2023cites this paper
• Discovery and pharmacological characterization of novel positive allosteric modulators acting on skeletal muscle-type nicotinic acetylcholine receptors.

  2023cites this paper
• Insights Into the Differential Desensitization of α4β2 Nicotinic Acetylcholine Receptor Isoforms Obtained With Positive Allosteric Modulation of Mutant Receptors

  2022cites this paper
• An experimental test of the nicotinic hypothesis of COVID-19

  2022cites this paper
• Cannabidiol as a modulator of α7 nicotinic receptors

  2022cites this paper
• Differential Activation and Desensitization States Promoted by Noncanonical α7 Nicotinic Acetylcholine Receptor Agonists

  2022cites this paper
• Acute effects of the imidacloprid metabolite desnitro-imidacloprid on human nACh receptors relevant for neuronal signaling

  2021cites this paper
• Therapeutic Targeting of a7 Nicotinic Acetylcholine Receptors

  2021influential citation
• Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors

  2021cites this paper
• Stable desensitization of α7 nicotinic acetylcholine receptors by NS6740 requires interaction with S36 in the orthosteric agonist binding site.

  2021cites this paper
• Neuronal Nicotinic Acetylcholine Receptors

  2021cites this paper
• The Allosteric Activation of α7 nAChR by α-Conotoxin MrIC Is Modified by Mutations at the Vestibular Site

  2021cites this paper
• Functional alterations by a subgroup of neonicotinoid pesticides in human dopaminergic neurons

  2021cites this paper
• The human-specific duplicated α7 gene inhibits the ancestral α7, negatively regulating nicotinic acetylcholine receptor-mediated transmitter release

  2021cites this paper
• Pharmacological Characterization of the Novel and Selective α7 Nicotinic Acetylcholine Receptor–Positive Allosteric Modulator BNC375

  2020cites this paper
• Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation.

  2020cites this paper
• Inhaled Aerosolized Nicotine Suppresses the Lung Eosinophilic Response to House Dust Mite Allergen.

  2020cites this paper
• Behavioral Pharmacology of the Cholinergic System

  2020influential citation
• Nicotinic receptor pharmacology in silico: Insights and challenges.

  2020cites this paper
• Activators of α7 nAChR as Potential Therapeutics for Cognitive Impairment.

  2020cites this paper
• Chemogenetics a Robust Approach to Pharmacology and Gene Therapy.

  2020cites this paper
• Nicotinic acetylcholine receptors: Conventional and unconventional ligands and signaling.

  2020cites this paper
• Implications of Oligomeric Amyloid-Beta (oAβ42) Signaling through α7β2-Nicotinic Acetylcholine Receptors (nAChRs) on Basal Forebrain Cholinergic Neuronal Intrinsic Excitability and Cognitive Decline

  2020cites this paper
• LL-00066471, a novel positive allosteric modulator of α7 nicotinic acetylcholine receptor ameliorates cognitive and sensorimotor gating deficits in animal models: Discovery and preclinical characterization.

  2020cites this paper
• Allosterically Potentiated a 7 Nicotinic Acetylcholine Receptors: Reduced Calcium Permeability and Current-Independent Control of Intracellular Calcium s

  2020influential citation
• The interplay between α7 nicotinic acetylcholine receptors, pannexin‐1 channels and P2X7 receptors elicit exocytosis in chromaffin cells

  2020cites this paper
• Allosterically Potentiated α7 Nicotinic Acetylcholine Receptors: Reduced Calcium Permeability and Current-Independent Control of Intracellular Calcium

  2020cites this paper
• Type I-like behavior of the type II α7 nicotinic acetylcholine receptor positive allosteric modulator A-867744

  2019cites this paper
• Binding Interactions of NS6740, a Silent Agonist of the α7 Nicotinic Acetylcholine Receptor

  2019cites this paper
• Heteromeric Neuronal Nicotinic Acetylcholine Receptors with Mutant β Subunits Acquire Sensitivity to α7-Selective Positive Allosteric Modulators

  2019influential citation
• Discovery of an intrasubunit nicotinic acetylcholine receptor–binding site for the positive allosteric modulator Br-PBTC

  2019cites this paper
• Isomerization of Asp7 in Beta-Amyloid Enhances Inhibition of the α7 Nicotinic Receptor and Promotes Neurotoxicity

  2019cites this paper
• Discovery of novel, potent, brain-permeable and orally efficacious positive allosteric modulator of alpha 7 nicotinic acetylcholine receptor [4-(5-(4-chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide], structure activity relationship and preclinical characterization.

  2019cites this paper
• Macroscopic and Microscopic Activation of α7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators (ago-PAMs) B-973B and GAT107

  2018cites this paper
• New Insights on Neuronal Nicotinic Acetylcholine Receptors as Targets for Pain and Inflammation: A Focus on α7 nAChRs

  2018cites this paper
• Designing selective modulators for the nicotinic receptor subtypes: challenges and opportunities.

  2018cites this paper
• Brain PET Imaging of α7-nAChR with [18F]ASEM: Reproducibility, Occupancy, Receptor Density, and Changes in Schizophrenia

  2018cites this paper
• Pharmacological modulation of the α7 nicotinic acetylcholine receptor in a mouse model of mecamylamine-precipitated nicotine withdrawal

  2018cites this paper
• Effect of nicotine and alpha‐7 nicotinic modulators on visceral pain‐induced conditioned place aversion in mice

  2018cites this paper
• Nicotinic acetylcholine receptors in neuropathic and inflammatory pain

  2018cites this paper
• Persistent activation of α7 nicotinic ACh receptors associated with stable induction of different desensitized states

  2018influential citation
• Orthosteric and allosteric potentiation of heteromeric neuronal nicotinic acetylcholine receptors

  2018influential citation
• The Antinociceptive and Anti-Inflammatory Properties of the α7 nAChR Weak Partial Agonist p-CF3 N,N-diethyl-N′-phenylpiperazine

  2018cites this paper
• Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the α7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation.

  2018cites this paper
• Macroscopic and Microscopic Activation of a 7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators ( ago-PAMs ) B-973 B and GAT 107 s

  2018cites this paper
• PET Brain imaging of α7-nAChR with [18F]ASEM

  2018cites this paper
• Counteracting desensitization of human α7-nicotinic acetylcholine receptors with bispyridinium compounds as an approach against organophosphorus poisoning.

  2017cites this paper
• Identification of α7 Nicotinic Acetylcholine Receptor Silent Agonists Based on the Spirocyclic Quinuclidine‐Δ2‐Isoxazoline Scaffold: Synthesis and Electrophysiological Evaluation

  2017cites this paper
• Design and Synthesis of Novel Allosteric Modulators of α7 Nicotinic Acetylcholine Receptor

  2017cites this paper
• Calcium imaging with genetically encoded sensor Case12: Facile analysis of α7/α9 nAChR mutants

  2017cites this paper
• The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator‐activated receptor‐&agr; represents a new antinociceptive signaling pathway in mice

  2017cites this paper
• B‐973, a novel piperazine positive allosteric modulator of the &agr;7 nicotinic acetylcholine receptor

  2017cites this paper
• Allosteric Modulation of Nicotinic Acetylcholine Receptors: The Concept and Therapeutic Trends.

  2016cites this paper
• Exploring the positive allosteric modulation of human α7 nicotinic receptors from a single-channel perspective.

  2016influential citation
• α7 nicotinic acetylcholine receptors: regulation of plasticity and network activity in the prelimbic cortex

  2016influential citation
• Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation

  2016cites this paper
• Neuronal Acetylcholine Nicotinic Receptors as New Targets for Lung Cancer Treatment.

  2016cites this paper
• Dissection of N,N-diethyl-N'-phenylpiperazines as α7 nicotinic receptor silent agonists.

  2016cites this paper
• Ligand Binding at the α4-α4 Agonist-Binding Site of the α4β2 nAChR Triggers Receptor Activation through a Pre-Activated Conformational State

  2016cites this paper
• Scopolamine-based pharmacological MRI model for testing procognitive agents

  2016cites this paper
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  2016influential citation
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  2016cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015influential citation
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  2015cites this paper
• Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor

  2015cites this paper
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  2015cites this paper
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  2014cites this paper
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  2014cites this paper
• Kinetic properties and open probability of α7 nicotinic acetylcholine receptors.

  2014influential citation
• The Minimal Pharmacophore for Silent Agonism of the α7 Nicotinic Acetylcholine Receptor

  2014cites this paper
• Mode of action of the positive modulator PNU-120596 on α7 nicotinic acetylcholine receptors.

  2014influential citation
• Allosteric Modulation as a Therapeutic Alternative to Orthosteric Activation in Nicotinic Acetylcholine Receptors

  2014cites this paper
• Nicotine increases GABAergic input on rat dorsal raphe serotonergic neurons through alpha7 nicotinic acetylcholine receptor.

  2014cites this paper
• Merging old and new perspectives on nicotinic acetylcholine receptors.

  2014cites this paper
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  2014cites this paper
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  2014cites this paper