SB-408124

288150-92-5

C19H18F2N4O

DMSO : 50 mg/mL (140.30 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

GPCR/G Protein; Neuronal Signaling

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. IC50 Value: 57 nM(Ki) Target: OX1 Receptor in vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production. in vivo: SB-408124 (30 ug/10 uL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 ug/10 uL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 uL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP).