Synthesis and biological activity of N-terminal lipidated and/or fluorescently labeled conjugates of astressin as corticotropin releasing factor antagonists Original Research Article

This report describes the synthesis of eight N-terminally modified astressin analogs and their biochemical evaluation as corticotropin releasing factor (CRF) antagonists. The lipidated astressin derivatives were tested on rat CRF receptor type 1 and 2α and were found to be active as CRF antagonists (rCRFR1: pA2 = 7.5–8.3; rCRFR2α: pA2 = 7.5–9.0) with nearly equal activities as compared to unmodified astressin (rCRFR1: pA2 = 8.3 ± 0.09; rCRFR2α: pA2 = 8.7 ± 0.08).