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

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 22, 2015, Pages 5111-5114

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

^a EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF ARKANSAS FOR MEDICAL SCIENCES   (United States)

Author keywords

Corticotropin releasing factor; CRF 1 receptor; Fluorine 18; PET imaging; Positron emission tomography

Indexed keywords

3 (6 DIMETHYLAMINO 4 METHYL 3 PYRIDINYL) 7 DIPROPYLAMINO 2,5 DIMETHYLPYRAZOLO[1,5 A]PYRIMIDINE; ALKYL GROUP; CARBON 11; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; FLUORINE 18; PYRAZINE DERIVATIVE; RADIOLIGAND; SAUVAGINE; TRACER; AMINOPYRIDINE DERIVATIVE; ANTISAUVAGINE 30; CORTICOTROPIN RELEASING FACTOR RECEPTOR; CORTICOTROPIN RELEASING FACTOR RECEPTOR 2; FLUORINE; FUSED HETEROCYCLIC RINGS; LIGAND; PEPTIDE FRAGMENT; RADIOPHARMACEUTICAL AGENT;

ARTICLE; BINDING AFFINITY; BRAIN UPTAKE; CONTROLLED STUDY; DRUG DEVELOPMENT; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG UPTAKE; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; ISOTOPE LABELING; LIPOPHILICITY; POSITRON EMISSION TOMOGRAPHY; ANIMAL; BRAIN; CELL LINE; CHEMISTRY; MACACA FASCICULARIS; MALE; METABOLISM; SYNTHESIS;

AMINOPYRIDINES; ANIMALS; BRAIN; CELL LINE; FLUORINE RADIOISOTOPES; HETEROCYCLIC COMPOUNDS, 2-RING; HUMANS; LIGANDS; MACACA FASCICULARIS; MALE; PEPTIDE FRAGMENTS; POSITRON-EMISSION TOMOGRAPHY; PYRAZINES; RADIOPHARMACEUTICALS; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE;

EID: 84945946835     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.10.010     Document Type: Article

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