Literature DB >> 23010264

[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.

Jeffrey A Deskus1, Douglas D Dischino, Ronald J Mattson, Jonathan L Ditta, Michael F Parker, Derek J Denhart, Dmitry Zuev, Hong Huang, Richard A Hartz, Vijay T Ahuja, Henry Wong, Gail K Mattson, Thaddeus F Molski, James E Grace, Larisa Zueva, Julia M Nielsen, Heidi Dulac, Yu-Wen Li, Mary Guaraldi, Michael Azure, David Onthank, Megan Hayes, Eric Wexler, Jennifer McDonald, Nicholas J Lodge, Joanne J Bronson, John E Macor.   

Abstract

Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET radioligand. Compound [(18)F]10 was prepared with high radiochemical purity and showed promising binding properties in rat brain imaging experiments.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23010264     DOI: 10.1016/j.bmcl.2012.08.112

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


  3 in total

1.  Synthesis, F-18 radiolabeling, and microPET evaluation of 3-(2,4-dichlorophenyl)-N-alkyl-N-fluoroalkyl-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-amines as ligands of the corticotropin-releasing factor type-1 (CRF1) receptor.

Authors:  Jeffrey S Stehouwer; Matthew S Birnbaum; Ronald J Voll; Michael J Owens; Susan J Plott; Chase H Bourke; Michael A Wassef; Clinton D Kilts; Mark M Goodman
Journal:  Bioorg Med Chem       Date:  2015-06-19       Impact factor: 3.641

2.  Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors.

Authors:  Nicholas J Lodge; Yu-Wen Li; Frederick T Chin; Douglas D Dischino; Sami S Zoghbi; Jeffrey A Deskus; Ronald J Mattson; Masao Imaizumi; Rick Pieschl; Thaddeus F Molski; Masahiro Fujita; Heidi Dulac; Robert Zaczek; Joanne J Bronson; John E Macor; Robert B Innis; Victor W Pike
Journal:  Nucl Med Biol       Date:  2014-03-29       Impact factor: 2.408

Review 3.  Corticotropin releasing hormone and imaging, rethinking the stress axis.

Authors:  Carlo Contoreggi
Journal:  Nucl Med Biol       Date:  2014-11-26       Impact factor: 2.408

  3 in total

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