CP 376395

"目录号: HY-14130

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CP 376395是有效和选择性的CRF1受体拮抗剂。

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生物活性

Description

CP 376395 is a potent and selectiveCorticotropin releasing factor 1 (CRF1)receptor antagonist.

IC50& Target

CRF1[1]

In Vitro

CP 376395 fully antagonizes oCRF-stimulated adenylate cyclase activity in rat cerebral cortex and at human CRF1 receptors with an apparent Kivalue 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[1].

In Vivo

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 ID50of 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[1].

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.