gsk-561679 and pyrazolopyridine

gsk-561679 has been researched along with pyrazolopyridine* in 1 studies

Other Studies

1 other study(ies) available for gsk-561679 and pyrazolopyridine

Article	Year
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. Bioorganic & medicinal chemistry letters, 2010, Dec-15, Volume: 20, Issue:24 Antagonists of the corticotropin-releasing factor (CRF) neuropeptide may prove effective in treating stress and anxiety related disorders. In an effort to identify antagonists with improved physico-chemical properties a new series of CRF(1) antagonists were designed to substitute the propyl groups at the C7 position of the pyrazolo[1,5-a]pyrimidine core of 1 with heterocycles. Compound (S)-8d was identified as a high affinity ligand with a pK(i) value of 8.2 and a functional CRF(1) antagonist with pIC(50) value of 7.0 in the in vitro CRF ACTH production assay. Topics: Azabicyclo Compounds; Humans; Microsomes, Liver; Oxadiazoles; Protein Binding; Pyrazoles; Pyridines; Receptors, Corticotropin-Releasing Hormone; Recombinant Proteins	2010

Article

Year

Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.

Bioorganic & medicinal chemistry letters, 2010, Dec-15, Volume: 20, Issue:24

Antagonists of the corticotropin-releasing factor (CRF) neuropeptide may prove effective in treating stress and anxiety related disorders. In an effort to identify antagonists with improved physico-chemical properties a new series of CRF(1) antagonists were designed to substitute the propyl groups at the C7 position of the pyrazolo[1,5-a]pyrimidine core of 1 with heterocycles. Compound (S)-8d was identified as a high affinity ligand with a pK(i) value of 8.2 and a functional CRF(1) antagonist with pIC(50) value of 7.0 in the in vitro CRF ACTH production assay.

Topics: Azabicyclo Compounds; Humans; Microsomes, Liver; Oxadiazoles; Protein Binding; Pyrazoles; Pyridines; Receptors, Corticotropin-Releasing Hormone; Recombinant Proteins

2010