143 articles for thisTarget
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BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
Bristol-Myers Squibb
Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] asa7 Nicotinic Receptor Agonists.
Bristol-Myers Squibb Research and Development
Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists.
Peking University
Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for thea3ß4 nicotinic acetylcholine receptor subtype.
Universit£
Recent developments in novel antidepressants targetinga4ß2-nicotinic acetylcholine receptors.
University of Illinois At Chicago
Dicarba analogues ofa-conotoxin RgIA. Structure, stability, and activity at potential pain targets.
Monash University (Parkville Campus)
Chalcones as positive allosteric modulators ofa7 nicotinic acetylcholine receptors: a new target for a privileged structure.
Instituto De Qu£Mica M£Dica (Iqm-Csic)
Semisynthetic analogues of toxiferine I and their pharmacological properties ata7 nAChRs, muscle-type nAChRs, and the allosteric binding site of muscarinic M2 receptors.
The German University In Cairo
Discovery of novel 2-((pyridin-3-yloxy)methyl)piperazines asa7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders.
Critical Therapeutics
Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists.
University of Copenhagen
Derivatives of dibenzothiophene for positron emission tomography imaging ofa7-nicotinic acetylcholine receptors.
The Johns Hopkins University School of Medicine
Characterization of a novela-conotoxin TxID from Conus textile that potently blocks rata3ß4 nicotinic acetylcholine receptors.
Hainan University
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.
University of Bonn
Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS): an allosteric agonist-positive allosteric modulator of α7 nicotinic acetylcholine receptors.
Northeastern University
Design, synthesis, and activity of a series of arylpyrid-3-ylmethanones as type I positive allosteric modulators of a7 nicotinic acetylcholine receptors.
University of California Irvine
Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor.
Targacept
Synthesis and evaluation of a conditionally-silent agonist for thea7 nicotinic acetylcholine receptor.
University of Florida
8-Benzamidochromen-4-one-2-carboxylic acids: potent and selective agonists for the orphan G protein-coupled receptor GPR35.
University of Bonn
Neonicotinic analogues: selective antagonists fora4ß2 nicotinic acetylcholine receptors.
University of Chile
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging ofa7 nicotinic acetylcholine receptors.
Helmholtz-Zentrum Dresden-Rossendorf
(+)-Laburnamine, a natural selective ligand and partial agonist for the?4?2 nicotinic receptor subtype.
Universit£
Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789).
Siena Biotech
Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.
Vu University Amsterdam
Deconstruction of thea4ß2 nicotinic acetylcholine receptor positive allosteric modulator desformylflustrabromine.
Virginia Commonwealth University
Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptora7 ligands.
Vu University Amsterdam
Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.
Glaxosmithkline
Discovery of (2S,3R)-N-[2-(Pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selectivea7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders.
Targacept
Discovery of highly potent and selectivea4ß2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
University of Illinois At Chicago
N-[5-(5-fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): a medicinal chemistry effort toward ana7 nicotinic acetylcholine receptor agonist preclinical candidate.
Siena Biotech
Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.
Targacept
Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selectivea4ß2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.
Targacept
Synthesis and nicotinic receptor activity of chemical space analogues of N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711).
University of Berne
Diazaspirocyclic compounds as selective ligands for thea4ß2 nicotinic acetylcholine receptor.
Targacept
The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement.
Glaxosmithkline
Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.
Glaxosmithkline
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.
Pfizer
Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.
Abbott Laboratories
Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist.
University of Copenhagen
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
University of Kentucky
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity.
Pfizer
Allosteric modulators of the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.
University of California
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
University of Copenhagen
Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors.
University of Florida
Synthesis and pharmacological characterization of exo-2-(2'-chloro-5-pyridinyl)-7-(endo and exo)-aminobicyclo[2.2.1]heptanes as novel epibatidine analogues.
Research Triangle Institute
3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation.
Pfizer
High affinity ligands for the alpha7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor.
Eli Lilly
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
The Danish University of Pharmaceutical Sciences
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Pfizer
2-(2-Piperidyl)- and 2-(2-pyrrolidyl)chromans as nicotine agonists: synthesis and preliminary pharmacological characterization.
University of Minnesota
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
Abbott Laboratories
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
Abbott Laboratories
Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the alpha3beta4* nicotinic acetylcholine receptors through modifications to the ester.
Ohio University
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
Astrazeneca
SAR ofa7 nicotinic receptor agonists derived from tilorone: exploration of a novel nicotinic pharmacophore.
Abbott Laboratories
Synthesis and binding affinity ata4ß2 anda7 nicotinic acetylcholine receptors of new analogs of epibatidine and epiboxidine containing the 7-azabicyclo[2.2.1]hept-2-ene ring system.
Universit£
New spirocyclic¿²-isoxazoline derivatives related to selective agonists ofa7 neuronal nicotinic acetylcholine receptors.
Universit£
Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors.
Vu University Amsterdam
Synthesis and biological activity of a novel class nicotinic acetylcholine receptors (nAChRs) ligands structurally related to anatoxin-a.
University of Ferrara
Discovery of non-peptide, small molecule antagonists ofa9a10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain.
University of Kentucky
Exploring a7-Nicotinic Receptor Ligand Diversity by Scaffold Enumeration from the Chemical Universe Database GDB.
TBA
Synthesis and structure-analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ).
Peking University
Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.
Abbott Laboratories
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
Pfizer
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis.
Institute
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Novartis Institutes For Biomedical Research
Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC).
Copenhagen University
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.
Amgen
Synthesis of poison-frog alkaloids 233A, 235U, and 251AA and their inhibitory effects on neuronal nicotinic acetylcholine receptors.
University of Toyama
Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.
Virginia Commonwealth University
Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.
University of Chile
Selective Penicillamine Substitution Enables Development of a Potent Analgesic Peptide that Acts through a Non-Opioid-Based Mechanism.
University of Utah
Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Bristol-Myers Squibb
Mechanism of Action and Structure-Activity Relationship of ?-Conotoxin Mr1.1 at the Human ?9?10 Nicotinic Acetylcholine Receptor.
Ocean University of China
From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human ?9?10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.
Universit£
Synthesis of full-length homodimer ?D-VxXXB that targets human ?7 nicotinic acetylcholine receptors.
The University of Queensland
6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model.
University of California
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human ?7 Nicotinic Acetylcholine Receptors.
Hainan University
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Emory University
Discovery of Methylene Thioacetal-Incorporated ?-RgIA Analogues as Potent and Stable Antagonists of the Human ?9?10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain.
University of Utah
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
University of Maryland
Novel Spiropiperidine Allosteric Modulators of Nicotinic Acetylcholine Receptors for Treating Central Nervous System Disorders.
Smith, Gambrell & Russell
Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of ?7 Nicotinic Acetylcholine Receptors.
Peking University
HTS-based discovery and optimization of novel positive allosteric modulators of the ?7 nicotinic acetylcholine receptor.
Gedeon Richter
Computational and Functional Mapping of Human and Rat ?6?4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs.
Veterans Affairs Medical Center
Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation.
University of Milan
Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups.
Consejo Superior De Investigaciones Cient�Ficas (Iqm-Csic)
Discovery of novel positive allosteric modulators of the ?7 nicotinic acetylcholine receptor: Scaffold hopping approach.
Gedeon Richter
5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors.
University of California
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as ?7 nicotinic receptor antagonists.
Peking University
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Bristol Myers Squibb Research and Development
Development of Conformationally Constrained ?-RgIA Analogues as Stable Peptide Antagonists of Human ?9?10 Nicotinic Acetylcholine Receptors.
University of Utah
Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds.
Mahidol University
Synthesis, Pharmacological Characterization, and Structure-Activity Relationships of Noncanonical Selective Agonists for ?7 nAChRs.
University of California-San Diego
New Rigid Nicotine Analogues, Carrying a Norbornane Moiety, Are Potent Agonists of ?7 and ?3* Nicotinic Receptors.
University of Florence
Medicinal properties of terpenes found in Cannabis sativa and Humulus lupulus.
Univerisity of Eastern Finland (Uef)
Discovery of fused heterocyclic carboxamide derivatives as novel ?7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation.
Peking University
Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.
Targacept
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.
Cea
Chemical conversion of nicotinamide into type I positive allosteric modulator of ?7 nAChRs.
Peking University
Discovery, cocrystallization and biological evaluation of novel piperidine derivatives as high affinity Ls-AChBP ligands possessing ?7 nAChR activities.
Fudan University
Structure and Activity Studies of Disulfide-Deficient Analogues of ?O-Conotoxin GeXIVA.
Hainan University
Dimerization of ?-Conotoxins as a Strategy to Enhance the Inhibition of the Human ?7 and ?9?10 Nicotinic Acetylcholine Receptors.
Ocean University of China
Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of ?7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization.
Lupin
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University of W£Rzburg
Di- and heptavalent nicotinic analogues to interfere with ?7 nicotinic acetylcholine receptors.
Universit£
Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.
Abbott Laboratories
Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the ?7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation.
University of Milan
Design and Synthesis of Novel Positive Allosteric Modulators of ?7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice.
Peking University
Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
University of California
Identification of novel ?7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric ?7 receptor ligand binding domain.
Bezmialem Vakif University
Potent Antiglioblastoma Agents by Hybridizing the Onium-Alkyloxy-Stilbene Based Structures of an ?7-nAChR, ?9-nAChR Antagonist and of a Pro-Oxidant Mitocan.
Universit£
Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine.
Indiana State University
Drimane Sesquiterpenoids Noncompetitively Inhibit Human ?4?2 Nicotinic Acetylcholine Receptors with Higher Potency Compared to Human ?3?4 and ?7 Subtypes.
California Northstate University College of Medicine
Allosteric Modulators of Nicotinic Acetylcholine Receptors Useful for the Treatment of Cognitive Impairment.
Temple University
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.
Amgen
Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the ?7 neuronal nicotinic receptor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Dual Nicotinic Acetylcholine Receptor ?4?2 Antagonists/?7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts.
University of Copenhagen
Development of spiroguanidine-derived?7 neuronal nicotinic receptor partial agonists.
Bristol-Myers Squibb Research and Development
Structure, synthesis and biological properties of the pentacyclic guanidinium alkaloids.
Nc State University
Sulfonium as a Surrogate for Ammonium: A New?7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.
University of Florida
New chemotypes as Trypanosoma cruzi triosephosphate isomerase inhibitors: a deeper insight into the mechanism of inhibition.
Universidad De La Republica
FABP1: A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein.
Avanti Polar Lipids
Cloning and functional expression of the guinea pig neuropeptide Y Y2 receptor.
Uppsala University