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Synthesis, Binding Affinity, Radiolabeling, and MicroPET Evaluation of 4-(2-Substituted-4-substituted)-8-(dialkylamino)-6-methyl-1-substituted-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-ones as Ligands for Brain Corticotropin-Releasing Factor Type-1 (CRF(1)) Receptors

Compounds 1–14 were synthesized in a search for high-affinity CRF(1) receptor ligands that could be radiolabeled with (11)C or (18)F for use as positron emission tomography (PET) radiotracers. Derivatives of 2 were developed which contained amide N-fluoroalkyl substituents. Compounds [(18)F]24 and [...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Stehouwer, Jeffrey S., Bourke, Chase H., Owens, Michael J., Voll, Ronald J., Kilts, Clinton D., Goodman, Mark M.
Formato: Artigo
Idioma:Inglês
Publicado em: 2015
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4628894/
https://ncbi.nlm.nih.gov/pubmed/26456805
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2015.10.010
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