| Description: |
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 be Fore Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and Forskolin-acivated cAMP production. SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) 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 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP). For the detailed information of SB-408124, the solubility of SB-408124 in water, the solubility of SB-408124 in DMSO, the solubility of SB-408124 in PBS buffer, the animal experiment (test) of SB-408124, the cell expriment (test) of SB-408124, the in vivo, in vitro and clinical trial test of SB-408124, the EC50, IC50,and Affinity of SB-408124, Please contact DC Chemicals. |
