Uses
CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist[1][2].
Biological Activity
Potent and selective CRF 1 receptor antagonist (K i values are 12 and >10000 nM for CRF 1 and CRF 2 receptors respectively). Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.
in vivo
CP 376395 (10-20 mg/kg, i.p., Male B6 mice) attenuates H2O and food intake, increases sucrose intake, attenuates EtOH intake but not EtOH preference[2].
| Animal Model: | Male B6 mice (n=8-9 per group)[2] |
| Dosage: | 0.0, 10.0, or 20.0 mg/kg |
| Administration: | Intraperitoneally
|
| Result: | Dose-dependently attenuated intake of H2O and food, with H2O intake affected specifically during the first half of the session. |
References
[1] Chen YL, et al. 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J Med Chem. 2008 Mar 13;51(5):1385-92. DOI:
10.1021/jm070579c[2] Giardino WJ, et al. CRF1 receptor signaling regulates food and fluid intake in the drinking-in-the-dark model of binge alcohol consumption. Alcohol Clin Exp Res. 2013 Jul;37(7):1161-70. DOI:
10.1111/acer.12076