1173523-48-2Relevant academic research and scientific papers
(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.
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists
Hartz, Richard A.,Ahuja, Vijay T.,Arvanitis, Argyrios G.,Rafalski, Maria,Yue, Eddy W.,Denhart, Derek J.,Schmitz, William D.,Ditta, Jonathan L.,Deskus, Jeffrey A.,Brenner, Allison B.,Hobbs, Frank W.,Payne, Joseph,Lelas, Snjezana,Li, Yu-Wen,Molski, Thaddeus F.,Mattson, Gail K.,Peng, Yong,Wong, Harvey,Grace, James E.,Lentz, Kimberley A.,Qian-Cutrone, Jingfang,Zhuo, Xiaoliang,Shu, Yue-Zhong,Lodge, Nicholas J.,Zaczek, Robert,Combs, Andrew P.,Olson, Richard E.,Bronson, Joanne J.,Mattson, Ronald J.,Macor, John E.
experimental part, p. 4173 - 4191 (2010/02/17)
Evidence suggests that corticotropin-releasing factor-1 (CRF1) receptor antagonistsmay offer therapeutic potential for the treatment of diseases associated with elevated levels of CRF such as anxiety and depression. A pyrazinone-based chemotype
