title: [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.
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.
authors.affiliation: Bristol-Myers Squibb Co., Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. jeffrey.deskus@bms.com
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Deskus
authors.forename: Douglas D
authors.initials: DD
authors.lastname: Dischino
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Mattson
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Ditta
authors.forename: Michael F
authors.initials: MF
authors.lastname: Parker
authors.forename: Derek J
authors.initials: DJ
authors.lastname: Denhart
authors.forename: Dmitry
authors.initials: D
authors.lastname: Zuev
authors.forename: Hong
authors.initials: H
authors.lastname: Huang
authors.forename: Richard A
authors.initials: RA
authors.lastname: Hartz
authors.forename: Vijay T
authors.initials: VT
authors.lastname: Ahuja
authors.forename: Henry
authors.initials: H
authors.lastname: Wong
authors.forename: Gail K
authors.initials: GK
authors.lastname: Mattson
authors.forename: Thaddeus F
authors.initials: TF
authors.lastname: Molski
authors.forename: James E
authors.initials: JE
authors.lastname: Grace
authors.forename: Larisa
authors.initials: L
authors.lastname: Zueva
authors.forename: Julia M
authors.initials: JM
authors.lastname: Nielsen
authors.forename: Heidi
authors.initials: H
authors.lastname: Dulac
authors.forename: Yu-Wen
authors.initials: YW
authors.lastname: Li
authors.forename: Mary
authors.initials: M
authors.lastname: Guaraldi
authors.forename: Michael
authors.initials: M
authors.lastname: Azure
authors.forename: David
authors.initials: D
authors.lastname: Onthank
authors.forename: Megan
authors.initials: M
authors.lastname: Hayes
authors.forename: Eric
authors.initials: E
authors.lastname: Wexler
authors.forename: Jennifer
authors.initials: J
authors.lastname: McDonald
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Lodge
authors.forename: Joanne J
authors.initials: JJ
authors.lastname: Bronson
authors.forename: John E
authors.initials: JE
authors.lastname: Macor
mesh_terms: D000814:Aniline Compounds / Q000737:chemistry*; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D005462:Fluorine Radioisotopes / Q000097:blood; D021621:Imaging, Three-Dimensional; D015394:Molecular Structure; D049268:Positron-Emission Tomography; D011719:Pyrazines / Q000737:chemistry*; D011720:Pyrazoles / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D014018:Tissue Distribution
chemical_list: C578926:(18F)(R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one; D000814:Aniline Compounds; D005462:Fluorine Radioisotopes; D011719:Pyrazines; D011720:Pyrazoles