Literature DB >> 19635669

Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies.

Idriss Bennacef1, Cristian A Salinas, Thomas A Bonasera, Roger N Gunn, Hélène Audrain, Steen Jakobsen, Nabeel Nabulsi, David Weinzimmer, Richard E Carson, Yiyun Huang, Ian Holmes, Fabrizio Micheli, Christian Heidbreder, Gabriella Gentile, Tino Rossi, Marc Laruelle.   

Abstract

Compound 1 is a potent and selective antagonist of the dopamine D(3) receptor. With the aim of developing a carbon-11 labeled ligand for the dopamine D(3) receptor, 1 was selected as a potential PET probe. [(11)C]1 was obtained by palladium catalyzed cross coupling using [(11)C]cyanide and 4 with a specific activity of 55.5+/-25.9GBq/micromol (1.5+/-0.7Ci/micromol). [(11)C]1 was tested in porcine and non-human primate models to assess its potential as a radioligand for PET imaging of the dopamine D(3) receptor. We conclude that in both species and despite appropriate in vitro properties, [(11)C]1 does not show any specific signal for the dopamine D(3) receptor.

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Year:  2009        PMID： 19635669     DOI： 10.1016/j.bmcl.2009.07.055

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: a positron emission tomography study.

Authors:  Robert H Mach; Zhude Tu; Jinbin Xu; Shihong Li; Lynne A Jones; Michelle Taylor; Robert R Luedtke; Colin P Derdeyn; Joel S Perlmutter; Mark A Mintun
Journal:  Synapse       Date:  2011-03-21       Impact factor: 2.562

2.  Effect of cyclosporin A on the uptake of D3-selective PET radiotracers in rat brain.

Authors:  Zhude Tu; Shihong Li; Jinbin Xu; Wenhua Chu; Lynne A Jones; Robert R Luedtke; Robert H Mach
Journal:  Nucl Med Biol       Date:  2011-03-03       Impact factor: 2.408

3.  Synthesis and pre-clinical evaluation of a potential radiotracer for PET imaging of the dopamine D3 receptor.

Authors:  Megan N Stewart; Xia Shao; Timothy J Desmond; Taylor J Forrest; Janna Arteaga; Jenelle Stauff; Peter J H Scott
Journal:  Medchemcomm       Date:  2018-06-29       Impact factor: 3.597

4.  [11C]Cyanation of arylboronic acids in aqueous solutions.

Authors:  Longle Ma; Michael S Placzek; Jacob M Hooker; Neil Vasdev; Steven H Liang
Journal:  Chem Commun (Camb)       Date:  2017-06-05       Impact factor: 6.222

Review 5.  Radiolabeling with [11C]HCN for Positron emission tomography.

Authors:  Yu-Peng Zhou; Katarina J Makaravage; Pedro Brugarolas
Journal:  Nucl Med Biol       Date:  2021-09-25       Impact factor: 2.408

Review 6.  Small Molecule Radiopharmaceuticals - A Review of Current Approaches.

Authors:  Shubhra Chaturvedi; Anil K Mishra
Journal:  Front Med (Lausanne)       Date:  2016-02-23
  6 in total

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