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Article Title

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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

Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.

Astrazeneca

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

Design, synthesis and binding affinity of acetylcholine carbamoyl analogues.

Universit£

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

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

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

Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.

Glaxosmithkline

Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4beta2 nicotinic ligands.

University Of Turin

3D-QSAR and QSSR studies of 3,8-diazabicyclo[4.2.0]octane derivatives as neuronal nicotinic acetylcholine receptors by comparative molecular field analysis (CoMFA).

Burnham Institute For Medical Research

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

alpha4beta2 nACh receptor pharmacophore models.

Virginia Commonwealth University

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

Discovery and development ofa7 nicotinic acetylcholine receptor modulators.

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

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

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

Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis.

Institute

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

Abbott Laboratories

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

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

Università

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

Synthesis and nicotinic receptor activity of a hydroxylated tropane.

University Of Wollongong

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

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

Conformationally restricted analogues of nicotine and anabasine.

Sibia Neurosciences

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

FABP1: A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein.

Avanti Polar Lipids

Structural and biochemical characterization of compounds inhibiting Mycobacterium tuberculosis pantothenate kinase.

Uppsala University

Novel Diketopiperazine Dihydroorotate Dehydrogenase Inhibitors Purified from Traditional Tibetan Animal Medicine Osteon Myospalacem Baileyi.

Chinese Academy Of Sciences