CP 316311 is a potent and selective CRF1 receptor antagonist with an IC50 value of 6.8 nM.
CP 316311 fully antagonizes CRF-stimulated adenylate cyclase activity in rat cortex and at human CRF1 receptors endogenously expressed in IMR32 cells with apparent Ki values of 7.6 and 8.5 nM, respectively[1].
CP 316311 (3.2 mg/kg) inhibits 125I-oCRF binding by >80% in rats. CP 316311 significantly attenuates activation of the hypothalamic-pituitary-adrenal (HPA) axis, with an MED value of 10 mg/kg, p.o. CP 316311 blocks the effects of both the exogenous and endogenous CRF in the CNS. CP 316311 blocks the effects induced by the exogeneous or endogeneous CRF in the brain in rat models[1].
[1]. Chen YL, et al. Synthesis and SAR of 2-aryloxy-4-alkoxy-pyridines as potent orally active corticotropin-releasing factor 1 receptor antagonists. J Med Chem. 2008 Mar 13;51(5):1377-84.