Literature DB >> 10100220

Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon.

J L Musachio1, V L Villemagne, U A Scheffel, R F Dannals, A S Dogan, F Yokoi, D F Wong.   

Abstract

A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (> 8,500 mCi/mumol). Preliminary single photon emission computed tomography studies with [123I]-5-IA in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [123I]-5-IA uptake in all brain regions (78-59% reduction), demonstrating the specificity of the radiotracer.

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Year:  1999        PMID： 10100220     DOI： 10.1016/s0969-8051(98)00101-2

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


  7 in total

1.  Persistent β2*-nicotinic acetylcholinergic receptor dysfunction in major depressive disorder.

Authors:  Aybala Saricicek; Irina Esterlis; Kathleen H Maloney; Yann S Mineur; Barbara M Ruf; Anjana Muralidharan; Jason I Chen; Kelly P Cosgrove; Rebecca Kerestes; Subroto Ghose; Carol A Tamminga; Brian Pittman; Frederic Bois; Gilles Tamagnan; John Seibyl; Marina R Picciotto; Julie K Staley; Zubin Bhagwagar
Journal:  Am J Psychiatry       Date:  2012-08       Impact factor: 18.112

2.  Human tobacco smokers in early abstinence have higher levels of beta2* nicotinic acetylcholine receptors than nonsmokers.

Authors:  Julie K Staley; Suchitra Krishnan-Sarin; Kelly P Cosgrove; Erica Krantzler; Erin Frohlich; Edward Perry; Joel A Dubin; Kristina Estok; Eric Brenner; Ronald M Baldwin; Gilles D Tamagnan; John P Seibyl; Peter Jatlow; Marina R Picciotto; Edythe D London; Stephanie O'Malley; Christopher H van Dyck
Journal:  J Neurosci       Date:  2006-08-23       Impact factor: 6.167

Review 3.  Imaging of cholinergic and monoaminergic neurochemical changes in neurodegenerative disorders.

Authors:  Nicolaas I Bohnen; Kirk A Frey
Journal:  Mol Imaging Biol       Date:  2007 Jul-Aug       Impact factor: 3.488

4.  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

5.  Stimulation of the alpha4beta2 nicotinic receptor by 5-I A-85380 improves auditory gating in DBA/2 mice.

Authors:  Kristin M Wildeboer; Karen E Stevens
Journal:  Brain Res       Date:  2008-06-11       Impact factor: 3.252

6.  Synthesis and evaluation of 3-¹²³I-iodo-5-[2-(S)-3-pyrrolinylmethoxy]-pyridine (niodene) as a potential nicotinic α4β2 receptor imaging agent.

Authors:  Suresh K Pandey; Shawn Pan; Ritu Kant; Sharon A Kuruvilla; Min-Liang Pan; Jogeshwar Mukherjee
Journal:  Bioorg Med Chem Lett       Date:  2012-10-10       Impact factor: 2.823

7.  Quantification of nicotinic acetylcholine receptors in human brain using [123I]5-I-A-85380 SPET.

Authors:  Masahiro Fujita; Masanori Ichise; Christopher H van Dyck; Sami S Zoghbi; Gilles Tamagnan; Alexey G Mukhin; Ali Bozkurt; Nicholas Seneca; Dnyanesh Tipre; Christopher C DeNucci; Hidehiro Iida; D Bruce Vaupel; Andrew G Horti; Andrei O Koren; Alane S Kimes; Edythe D London; John P Seibyl; Ronald M Baldwin; Robert B Innis
Journal:  Eur J Nucl Med Mol Imaging       Date:  2003-10-02       Impact factor: 9.236
  7 in total

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