Potent corticotropin-releasing factor (CRF)
receptor antagonist (Ki values are 2, 1.5 and 1 nM at CRF1,
CRF2α
and CRF2β).
Reduces ACTH secretion, blocks delayed gastric emptying and is neuroprotective
in vivo.
Gulyaset al (1995)
Potent, structurally constrained agonists and competitive antagonists of
corticotropin-releasing factor. Proc.Natl.Acad.Sci.USA 92 10575. Maeckeret al (1997) Astressin, a novel and potent CRF antagonist, is
neuroprotective in the hippocampus when administered after a seizure. Brain
Res. 744 166. Perrin and Vale(1999) Corticotropin
releasing factor receptors and their ligand family. Ann.N.Y.Acad.Sci. 885
312. Martinezet al (1999) Peripheral injection of a new
corticotropin-releasing factor (CRF) antagonist, astressin, blocks peripheral
CRF- and abdominal surgery-induced delayed gastric emptying in rats.
J.Pharmacol.Exp.Ther. 290 629.
Blocks CRF-induced adenylate cyclase activation (Ki = 3.7 nM) and attenuates activation of the HPA axis by CRF. Displays anxiolytic-like activity in the rat elevated plus-maze test; brain penetrant.