1408250-57-6Relevant articles and documents
(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
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 Jr., 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.
, p. 6651 - 6655 (2013/01/14)
Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET radioligand. Compound [18F]10 was prepared with high radiochemical purity and showed promising binding properties in rat brain imaging experiments.