Published in Mol Pharmacol on September 07, 2010
Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations. Biochem Pharmacol (2011) 1.68
Investigation of the molecular mechanism of the α7 nicotinic acetylcholine receptor positive allosteric modulator PNU-120596 provides evidence for two distinct desensitized states. Mol Pharmacol (2011) 1.37
The effective opening of nicotinic acetylcholine receptors with single agonist binding sites. J Gen Physiol (2011) 1.04
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. J Biol Chem (2013) 0.82
Covalent trapping of methyllycaconitine at the α4-α4 interface of the α4β2 nicotinic acetylcholine receptor: antagonist binding site and mode of receptor inhibition revealed. J Biol Chem (2013) 0.80
Potential state-selective hydrogen bond formation can modulate activation and desensitization of the α7 nicotinic acetylcholine receptor. J Biol Chem (2012) 0.77
Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION. J Biol Chem (2016) 0.76
Trapping of ivermectin by a pentameric ligand-gated ion channel upon open-to-closed isomerization. Sci Rep (2017) 0.75
Using CLUSTAL for multiple sequence alignments. Methods Enzymol (1996) 20.99
Nicotinic acetylcholine receptor alpha7 subunit is an essential regulator of inflammation. Nature (2002) 12.09
Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature (2001) 11.78
Structure and gating mechanism of the acetylcholine receptor pore. Nature (2003) 8.30
Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron (2004) 7.48
Substituted-cysteine accessibility method. Methods Enzymol (1998) 5.57
Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations. EMBO J (2005) 5.55
A glia-derived acetylcholine-binding protein that modulates synaptic transmission. Nature (2001) 3.69
Selective alpha7-nicotinic acetylcholine receptor agonist GTS-21 improves survival in murine endotoxemia and severe sepsis. Crit Care Med (2007) 3.63
The alpha7 nicotinic acetylcholine receptor as a pharmacological target for inflammation. Br J Pharmacol (2007) 2.82
Diversity of vertebrate nicotinic acetylcholine receptors. Neuropharmacology (2008) 2.49
Activation of the nicotinic acetylcholine receptor involves a switch in conformation of the alpha subunits. J Mol Biol (2002) 2.37
Heterogeneity and complexity of native brain nicotinic receptors. Biochem Pharmacol (2007) 2.37
Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis. Br J Pharmacol (2002) 2.34
Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc Natl Acad Sci U S A (2008) 2.20
Reactivity of small thiolate anions and cysteine-25 in papain toward methyl methanethiosulfonate. Biochemistry (1986) 2.20
Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol Pharmacol (2007) 1.98
Local stimulation of alpha7 cholinergic receptors inhibits LPS-induced TNF-alpha release in the mouse lung. Shock (2007) 1.59
Acetylcholine binding protein (AChBP): a secreted glial protein that provides a high-resolution model for the extracellular domain of pentameric ligand-gated ion channels. Annu Rev Biophys Biomol Struct (2003) 1.53
Neuronal nicotinic acetylcholine receptor expression and function on nonneuronal cells. AAPS J (2006) 1.52
Nicotine improves sustained attention in mice: evidence for involvement of the alpha7 nicotinic acetylcholine receptor. Neuropsychopharmacology (2004) 1.46
Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotine. J Pharmacol Exp Ther (2009) 1.33
alpha7 receptor-selective agonists and modes of alpha7 receptor activation. Eur J Pharmacol (2000) 1.31
Positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor: ligand interactions with distinct binding sites and evidence for a prominent role of the M2-M3 segment. Mol Pharmacol (2008) 1.23
Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptors. Mol Pharmacol (2008) 1.16
Characterization of the neuroprotective and toxic effects of alpha7 nicotinic receptor activation in PC12 cells. Brain Res (1999) 1.08
Cysteine accessibility analysis of the human alpha7 nicotinic acetylcholine receptor ligand-binding domain identifies L119 as a gatekeeper. Neuropharmacology (2010) 0.98
Probing the agonist domain of the nicotinic acetylcholine receptor by cysteine scanning mutagenesis reveals residues in proximity to the alpha-bungarotoxin binding site. Biochemistry (1999) 0.86
Mapping the agonist binding site of the nicotinic acetylcholine receptor by cysteine scanning mutagenesis: antagonist footprint and secondary structure prediction. Mol Pharmacol (2002) 0.85
Beta-estradiol attenuate amyloid beta-peptide toxicity via nicotinic receptors. Neuroreport (1999) 0.85
3H-nicotine- and 125I-alpha-bungarotoxin-labeled nicotinic receptors in the interpeduncular nucleus of rats. II. Effects of habenular deafferentation. J Comp Neurol (1986) 0.84
Mapping the structural requirements for nicotinic acetylcholine receptor activation by using tethered alkyltrimethylammonium agonists and antagonists. Biochemistry (2006) 0.84
Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations. Biochem Pharmacol (2011) 1.68
Investigation of the molecular mechanism of the α7 nicotinic acetylcholine receptor positive allosteric modulator PNU-120596 provides evidence for two distinct desensitized states. Mol Pharmacol (2011) 1.37
Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotine. J Pharmacol Exp Ther (2009) 1.33
Hydroxy metabolites of the Alzheimer's drug candidate 3-[(2,4-dimethoxy)benzylidene]-anabaseine dihydrochloride (GTS-21): their molecular properties, interactions with brain nicotinic receptors, and brain penetration. Mol Pharmacol (2004) 1.29
Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras. Neuropharmacology (2008) 1.25
Regulation of neuronal function by choline and 4OH-GTS-21 through alpha 7 nicotinic receptors. J Neurophysiol (2002) 1.23
The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors. Mol Pharmacol (2004) 1.18
Cytisine-based nicotinic partial agonists as novel antidepressant compounds. J Pharmacol Exp Ther (2009) 1.18
Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptors. Mol Pharmacol (2008) 1.16
Working with OpusXpress: methods for high volume oocyte experiments. Methods (2010) 1.14
Nicotinic receptors on local circuit neurons in dentate gyrus: a potential role in regulation of granule cell excitability. J Neurophysiol (2003) 1.11
Activation and inhibition of native neuronal alpha-bungarotoxin-sensitive nicotinic ACh receptors. Brain Res (2002) 1.10
Effects at a distance in alpha 7 nAChR selective agonists: benzylidene substitutions that regulate potency and efficacy. Neuropharmacology (2004) 1.07
Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptors. J Biol Chem (2006) 1.06
Neuronal nicotinic receptors as brain targets for pharmacotherapy of drug addiction. CNS Neurol Disord Drug Targets (2008) 1.05
The effective opening of nicotinic acetylcholine receptors with single agonist binding sites. J Gen Physiol (2011) 1.04
Intrinsically low open probability of α7 nicotinic acetylcholine receptors can be overcome by positive allosteric modulation and serum factors leading to the generation of excitotoxic currents at physiological temperatures. Mol Pharmacol (2012) 1.03
PATE gene clusters code for multiple, secreted TFP/Ly-6/uPAR proteins that are expressed in reproductive and neuron-rich tissues and possess neuromodulatory activity. J Biol Chem (2008) 1.02
Molecular dissection of tropisetron, an alpha7 nicotinic acetylcholine receptor-selective partial agonist. Neurosci Lett (2005) 1.02
An alpha7 nicotinic acetylcholine receptor gain-of-function mutant that retains pharmacological fidelity. Mol Pharmacol (2005) 0.98
Cysteine accessibility analysis of the human alpha7 nicotinic acetylcholine receptor ligand-binding domain identifies L119 as a gatekeeper. Neuropharmacology (2010) 0.98
Biochemical and functional properties of distinct nicotinic acetylcholine receptors in the superior cervical ganglion of mice with targeted deletions of nAChR subunit genes. Eur J Neurosci (2010) 0.96
Medial septal/diagonal band cells express multiple functional nicotinic receptor subtypes that are correlated with firing frequency. Neurosci Lett (2005) 0.95
Selective inhibition of acetylcholine-evoked responses of alpha7 neuronal nicotinic acetylcholine receptors by novel tris- and tetrakis-azaaromatic quaternary ammonium antagonists. Mol Pharmacol (2009) 0.94
Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor. Bioorg Med Chem Lett (2013) 0.94
α7β2 nicotinic acetylcholine receptors assemble, function, and are activated primarily via their α7-α7 interfaces. Mol Pharmacol (2011) 0.93
Multiple calcium channels and kinases mediate alpha7 nicotinic receptor neuroprotection in PC12 cells. J Neurochem (2005) 0.93
The effects of subunit composition on the inhibition of nicotinic receptors by the amphipathic blocker 2,2,6,6-tetramethylpiperidin-4-yl heptanoate. Mol Pharmacol (2005) 0.93
Differential regulation of receptor activation and agonist selectivity by highly conserved tryptophans in the nicotinic acetylcholine receptor binding site. J Pharmacol Exp Ther (2009) 0.93
Partial agonist and neuromodulatory activity of S 24795 for alpha7 nAChR responses of hippocampal interneurons. Neuropharmacology (2007) 0.92
Use of an α3β4 nicotinic acetylcholine receptor subunit concatamer to characterize ganglionic receptor subtypes with specific subunit composition reveals species-specific pharmacologic properties. Neuropharmacology (2012) 0.89
The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[3.2.2]nonane (TC-1698), a novel alpha7 ligand, is prevented through angiotensin II activation of a tyrosine phosphatase. J Pharmacol Exp Ther (2004) 0.89
Positive modulation of alpha7 nAChR responses in rat hippocampal interneurons to full agonists and the alpha7-selective partial agonists, 4OH-GTS-21 and S 24795. Neuropharmacology (2009) 0.88
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding. J Med Chem (2008) 0.88
Discovery of a novel nicotinic receptor antagonist for the treatment of nicotine addiction: 1-(3-Picolinium)-12-triethylammonium-dodecane dibromide (TMPD). Biochem Pharmacol (2007) 0.87
The nicotinic acetylcholine receptors of zebrafish and an evaluation of pharmacological tools used for their study. Biochem Pharmacol (2012) 0.87
In vivo characterization of a novel inhibitor of CNS nicotinic receptors. Eur J Pharmacol (2005) 0.86
A single point mutation confers properties of the muscle-type nicotinic acetylcholine receptor to homomeric alpha7 receptors. Mol Pharmacol (2004) 0.86
Differential modulation of brain nicotinic acetylcholine receptor function by cytisine, varenicline, and two novel bispidine compounds: emergent properties of a hybrid molecule. J Pharmacol Exp Ther (2013) 0.85
Diverse strategies targeting α7 homomeric and α6β2* heteromeric nicotinic acetylcholine receptors for smoking cessation. Ann N Y Acad Sci (2014) 0.84
Detecting extracellular carbonic anhydrase activity using membrane inlet mass spectrometry. Anal Biochem (2010) 0.84
Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors. Bioorg Med Chem Lett (2007) 0.83
The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion. Bioorg Med Chem Lett (2005) 0.83
Rhesus monkey alpha7 nicotinic acetylcholine receptors: comparisons to human alpha7 receptors expressed in Xenopus oocytes. Eur J Pharmacol (2005) 0.83
Multiple modes of α7 nAChR noncompetitive antagonism of control agonist-evoked and allosterically enhanced currents. Mol Pharmacol (2013) 0.82
Synthesis of H-bonding probes of alpha7 nAChR agonist selectivity. Bioorg Med Chem Lett (2008) 0.82
Functional central nicotinic acetylcholine receptor antagonism by systemic administration of Tinuvin 770 (BTMPS). Curr Alzheimer Res (2005) 0.82
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. J Biol Chem (2013) 0.82
Atypical antipsychotics as noncompetitive inhibitors of alpha4beta2 and alpha7 neuronal nicotinic receptors. Neuropharmacology (2009) 0.82
Free energy study of the catalytic mechanism of Trypanosoma cruzi trans-sialidase. From the Michaelis complex to the covalent intermediate. Biochemistry (2011) 0.82
Taurine-induced long-lasting potentiation in the rat hippocampus shows a partial dissociation from total hippocampal taurine content and independence from activation of known taurine transporters. J Neurochem (2004) 0.80
Septal innervation regulates the function of alpha7 nicotinic receptors in CA1 hippocampal interneurons. Exp Neurol (2005) 0.80
Identification of a gene cluster that initiates azasugar biosynthesis in Bacillus amyloliquefaciens. Chembiochem (2011) 0.79
The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2: carboxamide derivatives with different spacer motifs. Bioorg Med Chem (2013) 0.79
The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor (nAChR) ligands. Part 1: the influence of different hydrogen bond acceptor systems on alkyl and (hetero)aryl substituents. Bioorg Med Chem (2013) 0.79
Modulation of spontaneous hippocampal synaptic events with 5-hydroxyindole, 4OH-GTS-21, and rAAV-mediated alpha7 nicotinic receptor gene transfer. Brain Res (2008) 0.77
Potential state-selective hydrogen bond formation can modulate activation and desensitization of the α7 nicotinic acetylcholine receptor. J Biol Chem (2012) 0.77
Discovery of novel alpha7 nicotinic receptor antagonists. Bioorg Med Chem Lett (2010) 0.76
The cytisine derivatives, CC4 and CC26, reduce nicotine-induced conditioned place preference in zebrafish by acting on heteromeric neuronal nicotinic acetylcholine receptors. Psychopharmacology (Berl) (2014) 0.76
Point-to-point ligand-receptor interactions across the subunit interface modulate the induction and stabilization of conformational states of alpha7 nAChR by benzylidene anabaseines. Biochem Pharmacol (2013) 0.76
Similar activity of mecamylamine stereoisomers in vitro and in vivo. Eur J Pharmacol (2013) 0.76