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

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

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Published inBioorganic & medicinal chemistry letters Vol. 22; no. 21; pp. 6651 - 6655
Main Authors Deskus, Jeffrey A., Dischino, Douglas D., Mattson, Ronald J., Ditta, Jonathan L., Parker, Michael F., Denhart, Derek J., Zuev, Dmitry, Huang, Hong, Hartz, Richard A., Ahuja, Vijay T., Wong, Henry, Mattson, Gail K., Molski, Thaddeus F., Grace, James E., Zueva, Larisa, Nielsen, Julia M., Dulac, Heidi, Li, Yu-Wen, Guaraldi, Mary, Azure, Michael, Onthank, David, Hayes, Megan, Wexler, Eric, McDonald, Jennifer, Lodge, Nicholas J., Bronson, Joanne J., Macor, John E.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.11.2012
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
CORTICOTROPIN-RELEASING HORMONE
DEPRESSION
Antidepressants
CRF1
Positron Emission Tomography
Corticotropin-releasing factor
Radioligand
LIGAND
IN-VIVO EVALUATION
Anxiolytics
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Summary:Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET radioligand. Compound [F-18]10 was prepared with high radiochemical purity and showed promising binding properties in rat brain imaging experiments. (C) 2012 Elsevier Ltd. All rights reserved.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.08.112