(R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2, 5-dimethyl phenylamino)pyrazin-2(1H)-one: Introduction of N 3- phenylpyrazinones as potential CRF-R1 PET imaging agents

摘要

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.