SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with K i s of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor
In Vitro
Primary neuronal cultures from the hypothalamus of newborn SD rats are incubated with orexin A (1 µM), orexin A (1 µM) together with SB-408124 (100 µM) for 6 h. Orexin A-induced increases in arginine Vasotocin (AVP) mRNA levels (2.7-fold) are attenuated by SB-408124 (1.2-fold). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SB-408124 reduces anxiety after psychotraumatic exposure. Predator induces acute psychotraumatic exposure decrease corticoliberin level in the rat's amygdala. Intranasal administration of SB-408124 restores it closely to normal and has an anxiolytic effect on animal behaviour. Bilateral paraventricular nucleus microinjection of SB-408124 (30 pmol/50 nL per side) results in a greater reduction in mean arterial pressure (MAP) in high-salt intake (-16 mmHg) compared with NS-fed (-4 mmHg) anesthetized Dahl salt-sensitive rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:OX 1 Receptor 57 nM (Ki, in whole cell ) OX 1 Receptor 27 nM (Ki, in cell membrane)
