1260155-61-0Relevant articles and documents
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties
Tellew, John E.,Lanier, Marion,Moorjani, Manisha,Lin, Emily,Luo, Zhiyong,Slee, Deborah H.,Zhang, Xiaohu,Hoare, Sam R.J.,Grigoriadis, Dimitri E.,Denis, Yves St.,Fabio, Romano Di,Modugno, Enza Di,Saunders, John,Williams, John P.
scheme or table, p. 7259 - 7264 (2011/02/22)
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 CRF1 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 pKi value of 8.2 and a functional CRF1 antagonist with pIC50 value of 7.0 in the in vitro CRF ACTH production assay.
