265 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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a-Conotoxin [S9A]TxID Potently Discriminates betweena3ß4 anda6/a3ß4 Nicotinic Acetylcholine Receptors.
Hainan University
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
Bristol-Myers Squibb
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
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
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.
University of Milan
Design of novel 3,6-diazabicyclo[3.1.1]heptane derivatives with potent and selective affinities fora4ß2 neuronal nicotinic acetylcholine receptors.
University of Sassari
Synthesis, nicotinic acetylcholine receptor binding, in vitro and in vivo pharmacology properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs.
Research Triangle Institute
Bifunctional compounds targeting both D2 and non-a7 nACh receptors: design, synthesis and pharmacological characterization.
University of Milan
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.
University of Milan
Pharmacological profile of zacopride and new quaternarized fluorobenzamide analogues on mammaliana7 nicotinic acetylcholine receptor.
Orleans University
The twin drug approach for novel nicotinic acetylcholine receptor ligands.
University of Hawaii At Hilo
Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors.
University of Copenhagen
Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities ata7 nAChRs through incorporation of known structural motifs.
The University of Sydney
Investigations of amide bond variation and biaryl modification in analogues ofa7 nAChR agonist SEN12333.
The University of Sydney
Recent developments in novel antidepressants targetinga4ß2-nicotinic acetylcholine receptors.
University of Illinois At Chicago
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selectivea4ß2-nAChR Ligands.
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
Design ofa7 nicotinic acetylcholine receptor ligands in quinuclidine, tropane and quinazoline series. Chemistry, molecular modeling, radiochemistry, in vitro and in rats evaluations of a [(18)F] quinuclidine derivative.
Orleans University
Synthesis and pharmacological characterization of new neuronal nicotinic acetylcholine receptor ligands derived from Sazetidine-A.
Georgetown University Medical Center
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 binding affinity of acetylcholine carbamoyl analogues.
University of Milan
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
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 theα4β2 nicotinic receptor subtype.
University of Genoa
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
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 acetylcholine receptor in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues of 2'-fluoro-3'-(4-nitrophenyl)deschloroepibatidine.
Research Triangle Institute
Identification of novela4ß2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.
University of Illinois At Chicago
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
5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole as a potential PET radioligand for imaging cerebrala7-nAChR in mice.
The Johns Hopkins University School of Medicine
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
Consequences of linker length alteration of thea7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
The University of Sydney
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.
Pfizer
Novel tricyclic Delta(2)-isoxazoline and 3-oxo-2-methyl-isoxazolidine derivatives: synthesis and binding affinity at neuronal nicotinic acetylcholine receptor subtypes.
University of Milan
Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
Pfizer
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
Lycaconitine revisited: partial synthesis and neuronal nicotinic acetylcholine receptor affinities.
Ohio Northern University
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
Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine.
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
Parallel synthesis of a series of potentially brain penetrant aminoalkyl benzoimidazoles.
Siena Biotech
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
Synthesis and alpha4beta2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes.
University of Milan
Epibatidine isomers and analogues: structure-activity relationships.
University of Leicester
Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors.
Virginia Commonwealth University
(R)-3'-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties.
Mitsubishi Pharma
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
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
Mitsubishi Pharma
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors.
Pfizer
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists.
Research Triangle Institute
Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.
University of Kentucky
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
The Danish University of Pharmaceutical Sciences
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.
Pfizer
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist.
Research Triangle Institute
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
Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165.
Institut F£R Pharmazeutische Chemie Der Philipps-Universit£T Marburg
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues.
Research Triangle Institute
Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165.
University of Bath
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
Nudicauline and elatine as potent norditerpenoid ligands at rat neuronal alpha-bungarotoxin binding sites: importance of the 2-(methylsuccinimido)benzoyl moiety for neuronal nicotinic acetylcholine receptor binding.
School of Pharmacy and Pharmacology
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
University of Florida
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
N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors.
Chinese Academy of Sciences
bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors.
University of Kentucky
Neuronal nicotinic acetylcholine receptor binding affinities of boron-containing nicotine analogues.
University of Kentucky
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.
University of Milan
New spirocyclic¿²-isoxazoline derivatives related to selective agonists ofa7 neuronal nicotinic acetylcholine receptors.
University of Milan
Unichiral 2-(2'-pyrrolidinyl)-1,4-benzodioxanes: the 2R,2'S diastereomer of the N-methyl-7-hydroxy analogue is a potenta4ß2- anda6ß2-nicotinic acetylcholine receptor partial agonist.
University of Milan
Docking studies of benzylidene anabaseine interactions witha7 nicotinic acetylcholine receptor (nAChR) and acetylcholine binding proteins (AChBPs): application to the design of relateda7 selective ligands.
Targacept
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
Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
Targacept
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
Synthesis of novel chiral¿2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.
University of Milan
Novela3ß4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.
Sri International
Identification of 9-fluoro substituted (-)-cytisine derivatives as ligands with high affinity for nicotinic receptors.
Ensicaen-Université
A computational study of the binding of 3-(arylidene) anabaseines to two major brain nicotinic acetylcholine receptors and to the acetylcholine binding protein.
University of Florida
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
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, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-(substituted phenyl)epibatidine analogues. Nicotinic partial agonists.
Research Triangle Institute
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
Design of novel alpha7-subtype-preferring nicotinic acetylcholine receptor agonists: application of docking and MM-PBSA computational approaches, synthetic and pharmacological studies.
University of Milan
SAR and biological evaluation of SEN12333/WAY-317538: Novel alpha 7 nicotinic acetylcholine receptor agonist.
Wyeth Research
Tetrakis-azaaromatic quaternary ammonium salts: novel subtype-selective antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release.
University of Kentucky
Synthesis, binding, and modeling studies of new cytisine derivatives, as ligands for neuronal nicotinic acetylcholine receptor subtypes.
Università
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
5-(2-Pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes: synthesis of all the stereoisomers and alpha4beta2 nicotinic affinity.
Università
Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC).
Copenhagen University
Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for neuronal nicotinic acetylcholine receptors.
Università
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.
Amgen
Molecular engineering of conotoxins: the importance of loop size to alpha-conotoxin structure and function.
University of Queensland
Epiboxidine and novel-related analogues: a convenient synthetic approach and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.
Università
The synthesis of 5-substituted ring E analogs of methyllycaconitine via the Suzuki-Miyaura cross-coupling reaction.
Ohio University
Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands.
University of Florence
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
Optimization of Novel α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators and the Discovery of a Preclinical Development Candidate Molecule (RGH-560).
Gedeon Richter
Positive Allosteric Modulators of alpha7 Nicotinic Acetylcholine Receptor for the Treatment of Several Central Nervous System Diseases.
Therachem Research Medilab
Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.
University of Chile
Structure-Activity Relationships of Alanine Scan Mutants αO-Conotoxins GeXIVA[1,2] and GeXIVA[1,4].
Guangxi University
A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research.
Xiamen University
What We Have Gained from Ibogaine: α3β4 Nicotinic Acetylcholine Receptor Inhibitors as Treatments for Substance Use Disorders.
University of Illinois At Chicago
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.
Guangxi University
Subnanomolar Affinity and Selective Antagonism at α7 Nicotinic Receptor by Combined Modifications of 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624).
University of Milan
Synthesis, nicotinic acetylcholine receptor binding, antinociceptive and seizure properties of methyllycaconitine analogs.
Research Triangle Institute
Novel α7 nicotinic acetylcholine receptor modulators as potential antitussive agents.
Philip Morris International
Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.
University of Kentucky
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.
Pfizer
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 α-Conotoxin Mr1.1 at the Human α9α10 Nicotinic Acetylcholine Receptor.
Ocean University of China
From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.
University of Milan
The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.
University of Florida
Synthesis of full-length homodimer αD-VxXXB that targets human α7 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
Novel methyllycaconitine analogues selective for the α4β2 over α7 nicotinic acetylcholine receptors.
Australian National University
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human α7 Nicotinic Acetylcholine Receptors.
Hainan University
Synthesis and alpha4beta2 nicotinic affinity of 2-pyrrolidinylmethoxyimines and prolinal oxime ethers.
Università
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Emory University
Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain.
University of Utah
(+)-3-[2-(Benzo[b]thiophen-2-yl)-2-oxoethyl]-1-azabicyclo[2.2.2]octane as potent agonists for the alpha7 nicotinic acetylcholine receptor.
Mitsubishi Pharma
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
University of Maryland
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
University of Kentucky
Novel Spiropiperidine Allosteric Modulators of Nicotinic Acetylcholine Receptors for Treating Central Nervous System Disorders.
Smith, Gambrell & Russell
Chemical and functional identification and characterization of novel sulfated alpha-conotoxins from the cone snail Conus anemone.
The University of Queensland
Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors.
Peking University
HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor.
Gedeon Richter
Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity.
University of Bristol
Computational and Functional Mapping of Human and Rat α6β4 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.
IQM-CSIC
Discovery of novel positive allosteric modulators of the α7 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 α7 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
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent α4β2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the α3β4 Subtype.
University of Milan
Development of Conformationally Constrained α-RgIA Analogues as Stable Peptide Antagonists of Human α9α10 Nicotinic Acetylcholine Receptors.
University of Utah
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
Astrazeneca R&D Boston
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 α7 nAChRs.
University of California-San Diego
New Rigid Nicotine Analogues, Carrying a Norbornane Moiety, Are Potent Agonists of α7 and α3* 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 α7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation.
Peking University
Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.
Institute of Science and Technology
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 α7 nAChRs.
Peking University
Discovery, cocrystallization and biological evaluation of novel piperidine derivatives as high affinity Ls-AChBP ligands possessing α7 nAChR activities.
Fudan University
Structure and Activity Studies of Disulfide-Deficient Analogues of αO-Conotoxin GeXIVA.
Hainan University
PeIA-5466: A Novel Peptide Antagonist Containing Non-natural Amino Acids That Selectively Targets α3β2 Nicotinic Acetylcholine Receptors.
Veterans Affairs Medical Center
Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs.
Bionomics
Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors.
University of Sassari
Dimerization of α-Conotoxins as a Strategy to Enhance the Inhibition of the Human α7 and α9α10 Nicotinic Acetylcholine Receptors.
Ocean University of China
Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization.
Lupin
Bis(het)aryl-1,2,3-triazole quinuclidines as α7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [
Orleans University
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 α7 nicotinic acetylcholine receptors.
University of Nantes
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 α7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation.
University of Milan
Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice.
Peking University
Design of α7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies.
Universite Orleans
The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2: carboxamide derivatives with different spacer motifs.
University of Bonn
Anabaseine analogues as modulators of nicotinic acetylcholine receptor.
Dart Neuroscience
Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
University of California
Identification of novel α7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric α7 receptor ligand binding domain.
Bezmialem Vakif University
Structure-affinity relationships of a unique nicotinic ligand: N(1)-dimethyl-N(4)-phenylpiperazinium iodide (DMPP).
University of Florence
Synthesis and pharmacological characterization of [(125)I]iodomethyllycaconitine ([(125)I]iodo-MLA). A new ligand for the alpha(7) nicotinic acetylcholine receptor.
Research Triangle Institute
Potent Antiglioblastoma Agents by Hybridizing the Onium-Alkyloxy-Stilbene Based Structures of an α7-nAChR, α9-nAChR Antagonist and of a Pro-Oxidant Mitocan.
University of Milan
Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine.
Indiana State University
Drimane Sesquiterpenoids Noncompetitively Inhibit Human α4β2 Nicotinic Acetylcholine Receptors with Higher Potency Compared to Human α3β4 and α7 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
Single Amino Acid Substitution in α-Conotoxin TxID Reveals a Specific α3β4 Nicotinic Acetylcholine Receptor Antagonist.
Hainan University
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 α7 neuronal nicotinic receptor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α
Istituto Di Chimica Biomolecolare
Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts.
University of Copenhagen
Development of spiroguanidine-derivedα7 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 Newα7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.
University of Florida
Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.
Bayer Healthcare
Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.
Massachusetts Institute of Technology
The inhibitory effect of some new synthesized xanthates on mushroom tyrosinase activities.
University of Tehran
Agonist-induced up-regulation of alpha4beta2 nicotinic acetylcholine receptors in M10 cells: pharmacological and spatial definition.
University of Bath
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
Synaptic Pharmaceutical
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
National Institute of Mental Health
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Tufts University
Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
Universita Degli Studi Di Milano