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 (CRF1) receptors.

Jeffrey S Stehouwer,Michael J Owens,Chase H Bourke,Mark M Goodman,Ronald J Voll,Clinton D Kilts

doi:10.1016/j.bmcl.2015.10.010

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 (CRF1) receptors.

Jeffrey S Stehouwer, Michael J Owens + Show 4 more

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https://doi.org/10.1016/j.bmcl.2015.10.010

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Oct 8, 2015
Citations: 4	License type: elsevier-specific: oa user license

Affiliation: Emory University, University of Arkansas for Medical Sciences

#Corticotropin-releasing Factor Type-1 #microPET Imaging + Show 8 more

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Abstract

Compounds 1-14 were synthesized in a search for high-affinity CRF1 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 [(18)F]25 were found to have appropriate lipophilicities of logP7.4=2.2 but microPET imaging with [(18)F]25 demonstrated limited brain uptake.

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