Astressin 2B

Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying[1][2][3].

O=C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@](CC(C)C)(C)C(N[C@@H]([C@@H](C)CC)C(N)=O)=O)=O)=O)=O)=O)[C@@H](NC([C@@H](NC([C@H](C)NC([C@H](CCC(N)=O)NC([C@H](CCC(N)=O)NC([C@H](CCCCN)NC([C@H](CCC(O)=O)NC([C@H](CCCCN)NC([C@H](CCC(O)=O)NC([C@H](CCC(N)=O)NC([C@H](CCCCN)NC([C@H](CCC(O)=O)NC([C@H]([C@@H](C)CC)NC([C@H](CCC(O)=O)NC([C@H]([C@@H](C)CC)NC([C@H](CCCC)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@@](CC(C)C)(C)NC([C@H](CC1=CNC=N1)NC([C@@H](CC2=CC=CC=C2)NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CC(O)=O)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC(N[C@@H](CC(N)=O)C(N[C@H]3CC(N)=O)=O)=O)=O)CCCCNC3=O

[1]Rivier J, et al. Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. J Med Chem. 2002;45(21):4737-4747.|[2]Henry B, et al. The effect of lateral septum corticotropin-releasing factor receptor 2 activation on anxiety is modulated by stress. J Neurosci. 2006;26(36):9142-9152.|[3]Hoare SR, et al. Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupling sensitivity and determinants of CRF2 receptor selectivity. Peptides. 2005;26(3):457-470.