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. 2012 Nov 1;22(21):6651-5.
doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7.

[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 Deskus  1 , 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 Jr, 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
Affiliations

[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 Deskus et al. Bioorg Med Chem Lett. .

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.

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