Verucerfont

Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC₅₀s of ~6.1, >1000 and >1000?nM for CRF1, CRF2, and CRF-BP, respectively. IC50 & Target: IC50: 6.1 nM (CRF1), >1000 nM (CRF2), >1000 nM (CRF-BP)^[1] In Vivo: Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316?311, and pexacerfont (P<0.001 for all comparisons collapse across time-points); the latter three treatments in turn do not differ from each other. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, P<0.001). Accordingly, detailed Post hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6?h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline)^[1].