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[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.

Authors :
Deskus JA
Dischino DD
Mattson RJ
Ditta JL
Parker MF
Denhart DJ
Zuev D
Huang H
Hartz RA
Ahuja VT
Wong H
Mattson GK
Molski TF
Grace JE Jr
Zueva L
Nielsen JM
Dulac H
Li YW
Guaraldi M
Azure M
Onthank D
Hayes M
Wexler E
McDonald J
Lodge NJ
Bronson JJ
Macor JE
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Nov 01; Vol. 22 (21), pp. 6651-5. Date of Electronic Publication: 2012 Sep 07.
Publication Year :
2012

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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
22
Issue :
21
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
23010264
Full Text :
https://doi.org/10.1016/j.bmcl.2012.08.112