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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 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.

University of Milan

Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for thea3ß4 nicotinic acetylcholine receptor subtype.

University of Milan

Synthesis and pharmacological characterization of new neuronal nicotinic acetylcholine receptor ligands derived from Sazetidine-A.

Georgetown University Medical Center

Molecular basis of the selective binding of MDMA enantiomers to the alpha4beta2 nicotinic receptor subtype: synthesis, pharmacological evaluation and mechanistic studies.

University of Barcelona

Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists.

University of Copenhagen

Discovery of a potent and selectivea3ß4 nicotinic acetylcholine receptor antagonist from ana-conotoxin synthetic combinatorial library.

Torrey Pines Institute For Molecular Studies

Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling.

University of Milan

2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling.

National Institute On Drug Abuse

Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents.

University of Kentucky

Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.

University of Illinois At Chicago

Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.

Virginia Commonwealth University

Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.

Peking University

Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.

Abbott Laboratories

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine analogues.

Research Triangle Institute

Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.

Neurosearch

Syntheses and biological properties of cysteine-reactive epibatidine derivatives.

Louis Pasteur University

Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor.

R. W. Johnson Pharmaceutical Research Institute

From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.

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

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

Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties.

The Johns Hopkins University School of Medicine

Lycaconitine revisited: partial synthesis and neuronal nicotinic acetylcholine receptor affinities.

Ohio Northern University

Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists.

Research Triangle Institute

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

6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.

National Institute of Diabetes and Digestive and Kidney Diseases

Neuronal nicotinic acetylcholine receptors as targets for drug discovery.

Abbott Laboratories

Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.

Georgetown University School of Medicine

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

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

Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-(substituted phenyl)epibatidine analogues. Nicotinic partial agonists.

Research Triangle Institute

Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography.

The Johns Hopkins University School of Medicine

Tetrakis-azaaromatic quaternary ammonium salts: novel subtype-selective antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release.

University of Kentucky

 

Corrigendum to Epibatidine structureactivity relationships

TBA

Synthesis, binding, and modeling studies of new cytisine derivatives, as ligands for neuronal nicotinic acetylcholine receptor subtypes.

Università

Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.

Abbott Laboratories

5-(2-Pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes: synthesis of all the stereoisomers and alpha4beta2 nicotinic affinity.

Università

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

Epiboxidine and novel-related analogues: a convenient synthetic approach and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.

Università

Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands.

University of Florence

Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.

University of Kentucky

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 α4β2 nicotinic acetylcholine receptor ligands with different activity profiles at the two receptor stoichiometries.

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

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

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

Epibatidine structure-activity relationships.

Research Triangle Institute

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

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 biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists.

Peking University

Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors.

National Institute On Drug Abuse

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

Pyridine alkaloids with activity in the central nervous system.

University of Auckland

Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.

Abbott Laboratories

5-Azidoimidacloprid and an acyclic analogue as candidate photoaffinity probes for mammalian and insect nicotinic acetylcholine receptors.

University of California

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 α4β2 Receptor Antagonist for the Treatment of Depression.

Suven Life Sciences

(-)-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

Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.

Abbott Laboratories

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

Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors.

University of Sassari

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

Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.

IQM-CSIC

Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.

University of Copenhagen

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

Synthesis and evaluation of 3-¹²³I-iodo-5-[2-(S)-3-pyrrolinylmethoxy]-pyridine (niodene) as a potential nicotinic α4β2 receptor imaging agent.

University of California - Irvine

Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.

Abbott Laboratories

In silico characterization of cytisinoids docked into an acetylcholine binding protein.

Instituto De Investigaciones Biol£Gicas Clemente Estable

New ligands with affinity for the alpha4beta2 subtype of nicotinic acetylcholine receptors. Synthesis, receptor binding, and 3D-QSAR modeling.

Neurosearch

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

3-(2-Aminoethyl)pyridine analogs as alpha4beta2 nicotinic cholinergic receptor ligands.

Virginia Commonwealth University

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

Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.

The Bristol-Myers Squibb Pharmaceutical Research Institute

5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential probes for imaging with positron emission tomog

National Institute On Drug Abuse

Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.

Georgetown University Medical Center

3D QSAR analyses-guided rational design of novel ligands for the (alpha4)2(beta2)3 nicotinic acetylcholine receptor.

Institut F£R Pharmazeutische Chemie Der Philipps-Universit£T Marburg

Conformationally constrained nicotines: polycyclic, bridged, and spiro-annulated analogues as novel ligands for the nicotinic acetylcholine receptor.

Vienna University of Technology

Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes.

University of New Orleans

Structure-affinity relationships of a unique nicotinic ligand: N(1)-dimethyl-N(4)-phenylpiperazinium iodide (DMPP).

University of Florence

Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor.

University of California

Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine.

Indiana State University

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

From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism atα4β2 nicotinic acetylcholine receptor.

University of Milan

Highly Selective and Potentα4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.

Torrey Pines Institute For Molecular Studies

Nicotinic receptor compounds

Research Triangle Institute

Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes

Targacept

Viral polymerase inhibitors

Biota Scientific Management

Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.

Massachusetts Institute of Technology

Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed.

University of Copenhagen

Preparation and affinity profile of novel nicotinic ligands.

Servier, Chemistry Research Division A

7-Azaindole derivatives as potential partial nicotinic agonists.

Solvay Pharmaceuticals

Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs.

Research Triangle Institute

Heterologous expression of human {alpha}6{beta}4{beta}3{alpha}5 nicotinic acetylcholine receptors: binding properties consistent with their natural expression require quaternary subunit assembly including the {alpha}5 subunit.

Targacept

The comparative pharmacology and up-regulation of rat neuronal nicotinic receptor subtype binding sites stably expressed in transfected mammalian cells.

Georgetown University

Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.

The Danish University of Pharmaceutical Sciences

L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.

Case Western Reserve University

Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.

Case Western Reserve University

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories

5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors.

National Institute On Drug Abuse

Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.

Abbott Laboratories