Uses
BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM)[1].
Biochem/physiol Actions
BMS-665053 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 10 μM against 150 pM ovine CRF in binding assay). BMS-665053 exhibits anxiolytic efficacy in a defensive withdrawal anxiety test in rats in vivo (10 mg/kg p.o.) with good oral bioavailability (F = 52%).
References
[1] Jianqing Li, et al. An Efficient, Direct Bis-ortho-chlorination of 4-(Difluoromethoxy)aniline and Its Application to the Synthesis of BMS-665053, a Potent and Selective Pyrazinone-Containing Corticotropin-Releasing Factor-1 Receptor Antagonist. Organic Process Research & Development, 16, 156-159.
