Astressin 2B - HY-P1108

Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRF2, IC50 = 0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating Indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In a C. difficile toxin A-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is a valuable tool molecule for investigating the intestinal protective mechanisms of CRFR2[1][2][3][4][5][6][7].