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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

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

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

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

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

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

Glaxosmithkline

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

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

TBA

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

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

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

Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist.

University of Copenhagen

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

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

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

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 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

Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.

Hokkaido University

Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.

Barrow Neurological Institute

 

Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptor

TBA

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

Abbott Laboratories

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

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

Mechanism of Action and Structure-Activity Relationship of ?-Conotoxin Mr1.1 at the Human ?9?10 Nicotinic Acetylcholine Receptor.

Ocean University of China

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£

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

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 ?6?4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs.

Veterans Affairs Medical Center

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£

Pyridine alkaloids with activity in the central nervous system.

University of Auckland

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

New Rigid Nicotine Analogues, Carrying a Norbornane Moiety, Are Potent Agonists of ?7 and ?3* Nicotinic Receptors.

University of Florence

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

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

Alkaloids Purified from

American University of Health Sciences

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

Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the ?3?4 nicotinic acetylcholine receptor (nAChR).

Targacept

Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.

University of California

Differentiating the Pharmacodynamics and Toxicology of Macrolide and Ketolide Antibiotics.

Ponce De Leon Health

Structural basis for alpha-conotoxin potency and selectivity.

Boise State University

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

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

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

From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism at?4?2 nicotinic acetylcholine receptor.

Universit£

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

Chinese Academy of Sciences

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.

University of Leipzig