1.
ChemMedChem
; 3(2): 226-9, 2008 Feb.
Article
in English
| MEDLINE
| ID: mdl-18000940
Subject(s)
Anxiety/drug therapy , Depression/drug therapy , Drug Design , Pyrazoles/therapeutic use , Pyrimidines/therapeutic use , Receptors, Corticotropin-Releasing Hormone/antagonists & inhibitors , Animals , Anxiety/pathology , Corticotropin-Releasing Hormone/metabolism , Depression/pathology , Models, Chemical , Pyrazoles/chemical synthesis , Pyrazoles/pharmacokinetics , Pyrimidines/chemical synthesis , Pyrimidines/pharmacokinetics , Rats , Rats, Wistar , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 17(18): 5218-21, 2007 Sep 15.
Article
in English
| MEDLINE
| ID: mdl-17629700
ABSTRACT
Corticotropin-releasing factor (CRF), a 41 amino acid peptide neurohormone synthesised by specific hypothalamic nuclei in the brain, is implicated in stress-related function. Antagonism of CRF(1) receptors is an attractive therapeutic approach for the treatment of depression and anxiety. Unsaturated tetrahydrotriazaacenaphthylenes of general structure 3 have been identified as potent and selective CRF(1) receptor antagonists with a suitable oral pharmacokinetic profile.
