90 articles for thisTarget
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Article Title
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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
Synthesis and biological evaluation of novel hybrids of highly potent and selectivea4ß2-Nicotinic acetylcholine receptor (nAChR) partial agonists.
University of Illinois At Chicago
Novel 5-substituted 3-hydroxyphenyl and 3-nitrophenyl ethers of S-prolinol asa4ß2-nicotinic acetylcholine receptor ligands.
Universit£
Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for thea3ß4 nicotinic acetylcholine receptor subtype.
Universit£
The twin drug approach for novel nicotinic acetylcholine receptor ligands.
University of Hawaii At Hilo
Synthesis and pharmacological characterization of new neuronal nicotinic acetylcholine receptor ligands derived from Sazetidine-A.
Georgetown University Medical Center
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
Discovery of a potent and selectivea3ß4 nicotinic acetylcholine receptor antagonist from ana-conotoxin synthetic combinatorial library.
Torrey Pines Institute For Molecular Studies
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
University of Illinois At Chicago
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues.
Research Triangle Institute
Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.
Torrey Pines Institute For Molecular Studies
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
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Ucl School of Pharmacy
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
TBA
Diazaspirocyclic compounds as selective ligands for thea4ß2 nicotinic acetylcholine receptor.
Targacept
Discovery of Novel a4ß2 Neuronal Nicotinic Receptor Modulators through Structure-Based Virtual Screening.
TBA
Consequences of linker length alteration of thea7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
The University of Sydney
Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
The Danish University of Pharmaceutical Sciences
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.
University of Vermont
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
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
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Georgetown University School of Medicine
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
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
Novela3ß4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.
Sri International
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Barrow Neurological Institute
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
Pyrrolidinyl benzofurans and benzodioxanes: Selective ?4?2 nicotinic acetylcholine receptor ligands with different activity profiles at the two receptor stoichiometries.
Universit£
Posttranslational modifications of ?-conotoxins: sulfotyrosine and C-terminal amidation stabilise structures and increase acetylcholine receptor binding.
The University of Queensland
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£
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
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
University of Illinois At Chicago
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human ?7 Nicotinic Acetylcholine Receptors.
Hainan 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
Evaluation of ?-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
University of Jena
Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors.
University Hospital Hradec Kralove
Computational and Functional Mapping of Human and Rat ?6?4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs.
Veterans Affairs Medical Center
High Selectivity of an ?-Conotoxin LvIA Analogue for ?3?2 Nicotinic Acetylcholine Receptors Is Mediated by ?2 Functionally Important Residues.
Guangxi University
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
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D
University of Pennsylvania
Structure and Activity Studies of Disulfide-Deficient Analogues of ?O-Conotoxin GeXIVA.
Hainan University
PeIA-5466: A Novel Peptide Antagonist Containing Non-natural Amino Acids That Selectively Targets ?3?2 Nicotinic Acetylcholine Receptors.
Veterans Affairs Medical Center
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
Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.
Iqm-Csic
Synthesis and Pharmacological Evaluation of DH?E Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
University of Copenhagen
Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of ?3?4 nicotinic acetylcholine receptor.
Medical University of Lublin
Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the ?3?4 nicotinic acetylcholine receptor (nAChR).
Targacept
Differentiating the Pharmacodynamics and Toxicology of Macrolide and Ketolide Antibiotics.
Ponce De Leon Health
Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine.
Indian Institute of Technology
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
University of Illinois At Chicago
Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors.
Columbia University College of Physicians and Surgeons
Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking.
Swiss Federal Institute of Technology Zurich
6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.
Virginia Commonwealth University
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.
Georgetown University Medical Center
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
Single Amino Acid Substitution in ?-Conotoxin TxID Reveals a Specific ?3?4 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 ?7 neuronal nicotinic receptor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and biological activity of 5'-phenyl-1,2,5,6-tetrahydro-3,3'-bipyridine analogues as potential antagonists of nicotinic acetylcholine receptors.
University of Michigan
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£