[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

Autor:	Julia M. Nielsen, Jennifer McDonald, Dmitry Zuev, Megan Hayes, Eric Wexler, Joanne J. Bronson, Henry Wong, Yu-Wen Li, Nicholas J. Lodge, John E. Macor, Jeffrey A. Deskus, James E. Grace, Hong Huang, Gail K. Mattson, Mary Guaraldi, Derek J. Denhart, David C. Onthank, Vijay T. Ahuja, Heidi Dulac, Michael F. Parker, Larisa Zueva, Douglas D. Dischino, Ronald J. Mattson, Thaddeus F. Molski, Michael Azure, Jonathan L. Ditta, Richard A. Hartz
Rok vydání:	2012
Předmět:	Fluorine Radioisotopes Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry Medicinal chemistry Imaging Three-Dimensional Drug Discovery Radioligand Animals Tissue Distribution Molecular Biology Aniline Compounds Molecular Structure Chemistry Organic Chemistry Binding properties Brain Pet imaging Metabolic stability Rat brain Rats Positron-Emission Tomography Pyrazines Lipophilicity Pyrazoles Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 22:6651-6655
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2012.08.112
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e68bd4acd3bac602acb56267c782afe https://doi.org/10.1016/j.bmcl.2012.08.112 Zobrazit plný text záznamu Full Text from ScienceDirect