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Antisauvagine-30
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Sold with
the permission of the Max Planck Institute
Biological Activity:
Potent, selective and competitive corticotropin-releasing factor
CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM
for binding to mouse CRF2β and rat CRF1 receptors
respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells (pA2 = 8.49). Prevents
stress-enhanced fear conditioning and MEK 1/2-dependent activation of ERK1/2 in
mice in vivo.
Ruhmannet al (1998) Structural requirements for peptidic
antagonists of the corticotropin-releasing factor receptor (CRFR): development
of CRFR2β-selective antisauvagine-30. Proc.Natl.Acad.Sci.USA 95
15264. Braunset al (2001) Pharmacological and chemical
properties of astressin, antisauvagine-30 and α-helCRF: significance for
behavioral experiments. Neuropharmacology 41 507. Sananbenesiet al (2003) Mitogen-activated protein kinase signaling in the
hippocampus and its modulation by corticotropin-releasing factor receptor 2: a
possible link between stress and fear memory. J.Neurosci. 23
11436.
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.
