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A peptide CRF2 antagonist
Antisauvagine-30 is a peptide antagonist of corticotropin-releasing factor receptor 2 (CRF2).1,2 It is selective for CRF2α over CRF1 (Kis = 1.75 and 915 nM, respectively for the human receptors).1 Antisauvagine-30 (10 nM) inhibits sauvagine-induced cAMP production in HEK293 cells expressing mouse CRF2β.2 It prevents stress-induced contextual fear conditioning in mice.3 Antisauvagine-30 reduces vasoactive intestinal peptide-induced decreases in food intake in rats.4
1.Dautzenberg, F.M., Py-Lang, G., Higelin, J., et al.Different binding modes of amphibian and human corticotropin-releasing factor type 1 and type 2 receptors: Evidence for evolutionary differencesJ. Pharmacol. Exp. Ther.296(1)113-120(2001) 2.Rühmann, A., Bonk, I., Lin, C.R., et al.Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): Development of CRFR2β-selective antisauvagine-30Proc. Natl. Acad. Sci. USA95(26)15264-15269(1998) 3.Sananbenesi, F., Fischer, A., Schrick, C., et al.Mitogen-activated protein kinase signaling in the hippocampus and its modulation by corticotropin-releasing factor receptor 2: A possible link between stress and fear memoryJ. Neurosci.23(36)11436-11443(2003) 4.Garnica-Siqueira, M.C., Martins, A.B., Zaia, D.A.M., et al.Corticotrophin-releasing factor mediates vasoactive intestinal peptide-induced hypophagia and changes in plasma parametersHorm. Behav.105138-145(2018)
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