Molecular Formula | C21H30N2O |
Molar Mass | 326.48 |
Storage Condition | Desiccate at RT |
In vitro study | CP 376395 fully antagonizes oCRF-stimulated adenylate cyclase activity in rat cerebral cortex and at human CRF1 receptors with an apparent K i value of 12 nM, indicating antagonist functional activity. It is highly selective for the human CRF1 receptor subtype; affinity for the CRF2 receptor is >10000 nM. It shows affinities greater than 1 µM against 40 neurotransmitter receptor and ion channels. |
In vivo study | In the CNS, systemically administered CP 376395 blocks the effects of both exogenous and endogenous CRF. Pretreatment with CP 376395 reverses the excitation of locus coeruleus neurons induced by icv CRF (3 µg) with an ID 50 of completely blocked the enhanced startle response induced by icv CRF (1 µg) at 17.8 mg/kg, p.o. and partially blocked at 10 mg/kg, p.o. without significantly altering baseline startle. The attenuation of fear-potentiated startle is statistically significant at lower doses (0.32-3.2 mg/kg, p.o., with 62-83% blockade) and completely reversed by CP 376395 at 10 mg/kg, p.o. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.755 ml | 13.777 ml | 27.553 ml |
5 mM | 0.551 ml | 2.755 ml | 5.511 ml |
10 mM | 0.276 ml | 1.378 ml | 2.755 ml |
5 mM | 0.055 ml | 0.276 ml | 0.551 ml |
biological activity | CP 376395 is a potent and selective antagonist of the CRF1 receptor. |
Target | CRF1 |