TAK-875

溶解度:Soluble to 50 mM in DMSO and to 50 mM in ethanol

储存条件:Desiccate at +4°C

生物活性

Selective, non-peptide CRF₁ receptor antagonist (K_i values are 2.7 and > 10000 nM for CRF₁ and CRF₂ receptors respectively). Blocks CRF-induced adenylate cyclase activation (K_i = 3.7 nM) and attenuates activation of the HPA axis by CRF. Displays anxiolytic-like activity in the rat elevated plus-maze test; brain penetrant.

参考文献

Lundkist et al (1996) A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic activity. Eur.J.Pharmacol. 309 195. PMID: 8874139.

Schulz et al (1996) CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. Proc.Natl.Acad.Sci.USA 93 10477.

Hodgson et al (2007) Comparison of the V1b antagonist, SSR149415, and the CRF1 antagonist, CP-154,526, in rodent models of anxiety and depression. Pharmacol.Biochem.Behav. 86 431. PMID: 17291571.