BMS-763534 Chemische Eigenschaften,Einsatz,Produktion Methoden
Biochem/physiol Actions
BMS-763534 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 = 0.26 & 0.4 nM against 150 pM ovine CRF for binding rat & human CRF-R1, respectively), potency (IC50 = 1.0 nM against 0.3 nM CRF-stimulated ATCH secretion from primary rat anterior pituitary cells), and selectivity, displaying little affinity toward porcine CRF-R2/CRF2 and 46 other receptor/channel/transporter proteins (IC50 >10 μM). BMS-763534 inhibits CRF-stimulated cAMP production in human Y-79 retinoblastoma cells in cultures (pA2 = 9.47) and exhibits anxiolytic efficacy in a rat situational anxiety model in vivo (0.5-3 mg/kg p.o.).
BMS-763534 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte