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.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2007.06.077DOI Listing

Publication Analysis

Top Keywords

crf1 receptor
8
receptor antagonists
8
novel substituted
4
substituted tetrahydrotriazaacenaphthylene
4
tetrahydrotriazaacenaphthylene derivatives
4
derivatives potent
4
potent crf1
4
antagonists corticotropin-releasing
4
corticotropin-releasing factor
4
factor crf
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!