Literature DB >> 19481945

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.

Yongjun Gao1, Hayden T Ravert, Hiroto Kuwabara, Yingxian Xiao, Christopher J Endres, John Hilton, Daniel P Holt, Anil Kumar, Mohab Alexander, Dean F Wong, Robert F Dannals, Andrew G Horti.   

Abstract

The most abundant subtype of cerebral nicotinic acetylcholine receptors (nAChR), alpha4beta2, plays a critical role in various brain functions and pathological states. Imaging agents suitable for visualization and quantification of alpha4beta2 nAChRs by positron emission tomography (PET) would present unique opportunities to define the function and pharmacology of the nAChRs in the living human brain. In this study, we report the synthesis, nAChR binding affinity, and pharmacological properties of several novel 3-pyridyl ether compounds. Most of these derivatives displayed a high affinity to the nAChR and a high subtype selectivity for alpha4beta2-nAChR. Three of these novel nAChR ligands were radiolabeled with the positron-emitting isotope (11)C and evaluated in animal studies as potential PET radiotracers for imaging of cerebral nAChRs with improved brain kinetics.

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Year:  2009        PMID： 19481945      PMCID： PMC2719852          DOI： 10.1016/j.bmc.2009.05.021

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  38 in total

1.  In vivo imaging of human cerebral nicotinic acetylcholine receptors with 2-18F-fluoro-A-85380 and PET.

Authors:  Jean-Dominique Gallezot; Michel Bottlaender; Marie-Claude Grégoire; Dimitri Roumenov; Jean-Robert Deverre; Christine Coulon; Michèle Ottaviani; Frédéric Dollé; André Syrota; Héric Valette
Journal:  J Nucl Med       Date:  2005-02       Impact factor: 10.057

2.  Simplified quantification of nicotinic receptors with 2[18F]F-A-85380 PET.

Authors:  Sascha Mitkovski; Victor L Villemagne; Kathy E Novakovic; Graeme O'Keefe; Henri Tochon-Danguy; Rachel S Mulligan; Kerryn L Dickinson; Tim Saunder; Marie-Claude Gregoire; Michel Bottlaender; Frederic Dolle; Christopher C Rowe
Journal:  Nucl Med Biol       Date:  2005-08       Impact factor: 2.408

Review 3.  Central nicotinic receptors: structure, function, ligands, and therapeutic potential.

Authors:  M Novella Romanelli; Paola Gratteri; Luca Guandalini; Elisabetta Martini; Claudia Bonaccini; Fulvio Gualtieri
Journal:  ChemMedChem       Date:  2007-06       Impact factor: 3.466

Review 4.  Consensus nomenclature for in vivo imaging of reversibly binding radioligands.

Authors:  Robert B Innis; Vincent J Cunningham; Jacques Delforge; Masahiro Fujita; Albert Gjedde; Roger N Gunn; James Holden; Sylvain Houle; Sung-Cheng Huang; Masanori Ichise; Hidehiro Iida; Hiroshi Ito; Yuichi Kimura; Robert A Koeppe; Gitte M Knudsen; Juhani Knuuti; Adriaan A Lammertsma; Marc Laruelle; Jean Logan; Ralph Paul Maguire; Mark A Mintun; Evan D Morris; Ramin Parsey; Julie C Price; Mark Slifstein; Vesna Sossi; Tetsuya Suhara; John R Votaw; Dean F Wong; Richard E Carson
Journal:  J Cereb Blood Flow Metab       Date:  2007-05-09       Impact factor: 6.200

Review 5.  Neuronal nicotinic acetylcholine receptors as targets for drug discovery.

Authors:  M W Holladay; M J Dart; J K Lynch
Journal:  J Med Chem       Date:  1997-12-19       Impact factor: 7.446

6.  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.

Authors:  F Doll; L Dolci; H Valette; F Hinnen; F Vaufrey; I Guenther; C Fuseau; C Coulon; M Bottlaender; C Crouzel
Journal:  J Med Chem       Date:  1999-06-17       Impact factor: 7.446

Review 7.  Neuronal nicotinic receptors in the human brain.

Authors:  D Paterson; A Nordberg
Journal:  Prog Neurobiol       Date:  2000-05       Impact factor: 11.685

8.  Evaluation of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine and its analogues as PET radioligands for imaging nicotinic acetylcholine receptors.

Authors:  LaVerne Brown; Svetlana Chefer; Olga Pavlova; D Bruce Vaupel; Andrei O Koren; Alane S Kimes; Andrew G Horti; Alexey G Mukhin
Journal:  J Neurochem       Date:  2004-11       Impact factor: 5.372

9.  Human striatal L-dopa decarboxylase activity estimated in vivo using 6-[18F]fluoro-dopa and positron emission tomography: error analysis and application to normal subjects.

Authors:  H Kuwabara; P Cumming; J Reith; G Léger; M Diksic; A C Evans; A Gjedde
Journal:  J Cereb Blood Flow Metab       Date:  1993-01       Impact factor: 6.200

Review 10.  Development of radioligands with optimized imaging properties for quantification of nicotinic acetylcholine receptors by positron emission tomography.

Authors:  Andrew G Horti; Yongjun Gao; Hiroto Kuwabara; Robert F Dannals
Journal:  Life Sci       Date:  2009-03-18       Impact factor: 5.037
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  2 in total

1.  Clinical Perspective and Recent Development of PET Radioligands for Imaging Cerebral Nicotinic Acetylcholine Receptors.

Authors:  Andrew G Horti; Dean F Wong
Journal:  PET Clin       Date:  2009-01-01

2.  Competition, Selectivity and Efficacy of Analogs of A-84543 for Nicotinic Acetylcholine Receptors with Repositioning of Pyridine Nitrogen.

Authors:  Adebowale E Ogunjirin; Joseph M Fortunak; LaVerne L Brown; Yingxian Xiao; Martha I Dávila-García
Journal:  Neurochem Res       Date:  2015-10-27       Impact factor: 3.996
  2 in total

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