Literature DB >> 11003056

6-[18F]fluoro-A-85380, a novel radioligand for in vivo imaging of central nicotinic acetylcholine receptors.

A G Horti1, S I Chefer, A G Mukhin, A O Koren, D Gündisch, J M Links, V Kurian, R F Dannals, E D London.   

Abstract

A novel positron emission tomography (PET) radiotracer, 6-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (6-[18F]fluoro-A-85380, 6-[18F]FA) was synthesized by a no-carrier-added fluorination. In vitro 6-[18F]FA bound to nicotinic acetylcholine receptors (nAChRs), with very high affinity (Kd 28 pM). In PET studies, 6-[18F]FA specifically labeled central nAChRs in the brain of the Rhesus monkey and demonstrated highest levels of accumulation of radioactivity in brain regions enriched with the alpha4beta2 subtype of nAChR. 6-[18F]FA exhibited a target-to-non-target ratio (estimated as radioactivity in the thalamus to that in the cerebellum) of binding in primate brain similar to that previously determined for a labeled analog of epibatidine, [18F]FPH. In contrast to [18F]FPH, the novel tracer is expected to exhibit substantially less toxicity. Thus, the novel radioligand, 6-[18F]FA, appears to be a suitable candidate for imaging nAChRs in human brain.

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Year:  2000        PMID： 11003056     DOI： 10.1016/s0024-3205(00)00635-4

Source DB:  PubMed          Journal:  Life Sci        ISSN： 0024-3205            Impact factor:   5.037


  7 in total

1.  Selective syntheses of no-carrier-added 2- and 3-[18F]fluorohalopyridines through the radiofluorination of halopyridinyl(4'-methoxyphenyl)iodonium tosylates.

Authors:  Joong-Hyun Chun; Victor W Pike
Journal:  Chem Commun (Camb)       Date:  2012-08-30       Impact factor: 6.222

2.  Quantification of smoking-induced occupancy of beta2-nicotinic acetylcholine receptors: estimation of nondisplaceable binding.

Authors:  Irina Esterlis; Kelly P Cosgrove; Jeffery C Batis; Frederic Bois; Stephanie M Stiklus; Evgenia Perkins; John P Seibyl; Richard E Carson; Julie K Staley
Journal:  J Nucl Med       Date:  2010-07-21       Impact factor: 10.057

3.  Single photon emission computed tomography experience with (S)-5-[(123)I]iodo-3-(2-azetidinylmethoxy)pyridine in the living human brain of smokers and nonsmokers.

Authors:  James Robert Brasić; Yun Zhou; John L Musachio; John Hilton; Hong Fan; Andrew Crabb; Christopher J Endres; Melvin J Reinhardt; Ahmet S Dogan; Mohab Alexander; Olivier Rousset; Marika A Maris; Jeffrey Galecki; Ayon Nandi; Dean F Wong
Journal:  Synapse       Date:  2009-04       Impact factor: 2.562

4.  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.

Authors:  Yongjun Gao; 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
Journal:  Bioorg Med Chem       Date:  2009-05-15       Impact factor: 3.641

5.  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

Review 6.  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

Review 7.  PET Imaging of the Human Nicotinic Cholinergic Pathway in Atherosclerosis.

Authors:  Matthias Bauwens; Felix M Mottaghy; Jan Bucerius
Journal:  Curr Cardiol Rep       Date:  2015-08       Impact factor: 2.931
  7 in total

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