130 articles for thisTarget
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Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of novel hybrids of highly potent and selectivea4ß2-Nicotinic acetylcholine receptor (nAChR) partial agonists.
University of Illinois At Chicago
Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for thea3ß4 nicotinic acetylcholine receptor subtype.
Universit£
Design of novel 3,6-diazabicyclo[3.1.1]heptane derivatives with potent and selective affinities fora4ß2 neuronal nicotinic acetylcholine receptors.
University of Sassari
Exploration of the molecular architecture of the orthosteric binding site in thea4ß2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.
University of Copenhagen
Bifunctional compounds targeting both D2 and non-a7 nACh receptors: design, synthesis and pharmacological characterization.
Universit£
Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed asa4ß2-Nicotinic Acetylcholine Receptor Agonists.
Universit£
The twin drug approach for novel nicotinic acetylcholine receptor ligands.
University of Hawaii At Hilo
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
Synthesis and activity of substituted heteroaromatics as positive allosteric modulators fora4ß2a5 nicotinic acetylcholine receptors.
The Scripps Research Institute
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
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.
Georgetown University
2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.
Virginia Commonwealth University
QM-polarized ligand docking accurately predicts the trend in binding affinity of a series of arylmethylene quinuclidine-like derivatives at thea4ß2 anda3ß4 nicotinic acetylcholine receptors (nAChRs).
Targacept
Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: pharmacophore modeling and structure-activity relationship studies.
The Ohio State University
Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selectivea4ß2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II.
University of Illinois At Chicago
Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor.
Targacept
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Ucl School of Pharmacy
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
Discovery of a novel series of quinolonea7 nicotinic acetylcholine receptor agonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
(+)-Laburnamine, a natural selective ligand and partial agonist for the?4?2 nicotinic receptor subtype.
Universit£
Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selectivea4ß2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats.
Georgetown University Medical Center
Synthesis, pharmacology, and biostructural characterization of novela4ß2 nicotinic acetylcholine receptor agonists.
University of Copenhagen
3D-QSAR and 3D-QSSR models of negative allosteric modulators facilitate the design of a novel selective antagonist of humana4ß2 neuronal nicotinic acetylcholine receptors.
The Ohio State University
Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.
Vu University Amsterdam
Discovery of novela7 nicotinic acetylcholine receptor ligands via pharmacophoric and docking studies of benzylidene anabaseine analogs.
Targacept
Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.
The Ohio State University
Deconstruction of thea4ß2 nicotinic acetylcholine receptor positive allosteric modulator desformylflustrabromine.
Virginia Commonwealth University
Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) asa4ß2-nicotinic acetylcholine receptor-selective partial agonists.
University of Illinois At Chicago
Unique spirocyclopiperazinium salt III: further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics.
Peking University
Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine.
Research Triangle Institute
Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists.
Neuroscience Research
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.
Abbott Laboratories
Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists.
Abbott Laboratories
Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes.
Research Triangle Institute
Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Peking University
A novel nicotinic acetylcholine receptor antagonist radioligand for PET studies.
Brookhaven National Laboratory
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
3-(4-Aminobutyn-1-yl)pyridines: binding at alpha 4 beta 2 nicotinic cholinergic receptors.
Virginia Commonwealth University
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
TBA
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
Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.
Targacept
Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands toa4ß2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands.
University of Illinois At Chicago
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
Chemistry and behavioral studies identify chiral cyclopropanes as selectivea4ß2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile.
University of Illinois At Chicago
Discovery of Novel a4ß2 Neuronal Nicotinic Receptor Modulators through Structure-Based Virtual Screening.
TBA
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
Nicotinic Acetylcholine Receptor Efficacy and Pharmacological Properties of 3-(Substituted phenyl)-2ß-substituted Tropanes.
Research Triangle Institute
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
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
Epibatidine isomers and analogues: structure-activity relationships.
University of Leicester
Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors.
Virginia Commonwealth University
3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation.
Pfizer
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
The Danish University of Pharmaceutical Sciences
2-(Arylmethyl)-3-substituted quinuclidines as selective alpha 7 nicotinic receptor ligands.
Targacept
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Pfizer
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
(S)-(-)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): a novel anti-parkinsonian agent with selectivity for neuronal nicotinic acetylcholine receptors.
Sibia Neurosciences
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
University of Florida
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth 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£
Discovery of isoxazole analogues of sazetidine-A as selectivea4ß2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.
University of Illinois At Chicago
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 of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.
Research Triangle Institute
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
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Barrow Neurological Institute
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Siena Biotech
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.
Research Triangle Institute
Novel 2-(2′-furo[3,2-b]pyridinyl) pyrrolidines: potent neuronal nicotinic acetylcholine receptor ligands
TBA
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
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
University College London
Pyrrolidinyl benzofurans and benzodioxanes: Selective ?4?2 nicotinic acetylcholine receptor ligands with different activity profiles at the two receptor stoichiometries.
Universit£
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£
Novel methyllycaconitine analogues selective for the ?4?2 over ?7 nicotinic acetylcholine receptors.
Australian National 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
Synthesis and nicotinic receptor activity of a hydroxylated tropane.
University of Wollongong
Computational and Functional Mapping of Human and Rat ?6?4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs.
Veterans Affairs Medical Center
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
Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors.
University of California
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent ?4?2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the ?3?4 Subtype.
Universit£
Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine ?4?2 Receptor Antagonist for the Treatment of Depression.
Suven Life Sciences
Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds.
Mahidol University
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
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors.
Universit£
Philanthotoxin Analogues That Selectively Inhibit Ganglionic Nicotinic Acetylcholine Receptors with Exceptional Potency.
University of Nottingham
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Abbott Laboratories
Bis(het)aryl-1,2,3-triazole quinuclidines as ?7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [
Universit£
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University of W£Rzburg
Design of ?7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies.
Universite Orleans
Identification and pharmacological characterization of 3,6-diazabicyclo[3.1.1]heptane-3-carboxamides as novel ligands for the ?4?2 and ?6/?3?2?3 nicotinic acetylcholine receptors (nAChRs).
Targacept
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
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.
Amgen
Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for ?
Istituto Di Chimica Biomolecolare
Dual Nicotinic Acetylcholine Receptor ?4?2 Antagonists/?7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts.
University of Copenhagen
From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism at?4?2 nicotinic acetylcholine receptor.
Universit£