Literature DB >> 10755645

6-[18F]Fluoro-A-85380: an in vivo tracer for the nicotinic acetylcholine receptor.

U Scheffel1, A G Horti, A O Koren, H T Ravert, J P Banta, P A Finley, E D London, R F Dannals.   

Abstract

6-[18F]Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (6-[18F]fluoro-A-85380 or 6-[18F]FA), a new tracer for positron emission tomography, was synthesized by no-carrier-added [18F] fluorination of 6-iodo-3-((1-tert-butoxycarbonyl-2(S)-azetidinyl)methoxy)pyridine followed by acidic deprotection. 6-[18F]FA followed the regional densities of brain nicotinic acetylcholine receptors (nAChRs) reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 6-FA. A preliminary toxicology study of the 6-FA showed a relatively low biological effect.

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Year:  2000        PMID： 10755645     DOI： 10.1016/s0969-8051(99)00082-7

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN： 0969-8051            Impact factor:   2.408


  4 in total

1.  Beta-amyloid activates the mitogen-activated protein kinase cascade via hippocampal alpha7 nicotinic acetylcholine receptors: In vitro and in vivo mechanisms related to Alzheimer's disease.

Authors:  K T Dineley; M Westerman; D Bui; K Bell; K H Ashe; J D Sweatt
Journal:  J Neurosci       Date:  2001-06-15       Impact factor: 6.167

2.  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

3.  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 4.  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
  4 in total

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