Synthesis and biological activity of N-terminal lipidated and/or fluorescently labeled conjugates of astressin as corticotropin releasing factor antagonists
摘要:
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 2alpha and were found to be active as CRF antagonists (rCRFR1: pA(2) = 7.5-8.3; rCRFR2alpha: pA(2) = 7.5-9.0) with nearly equal activities as compared to unmodified astressin (rCRFR1: pA(2) = 8.3 +/- 0.09; rCRFR2alpha: pA(2) = 8.7 +/- 0.08). (C) 2004 Elsevier Ltd. All rights reserved.
Synthesis and biological activity of N-terminal lipidated and/or fluorescently labeled conjugates of astressin as corticotropin releasing factor antagonists
摘要:
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 2alpha and were found to be active as CRF antagonists (rCRFR1: pA(2) = 7.5-8.3; rCRFR2alpha: pA(2) = 7.5-9.0) with nearly equal activities as compared to unmodified astressin (rCRFR1: pA(2) = 8.3 +/- 0.09; rCRFR2alpha: pA(2) = 8.7 +/- 0.08). (C) 2004 Elsevier Ltd. All rights reserved.