产品
编 号:F161419
分子式:C19H19ClF2N4O
分子量:392.83
产品类型
结构图
CAS No: 1431697-90-3
联系客服
产品详情
生物活性:
SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor.
体内研究:
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.
体外研究:
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 vasopressin (AVP) mRNA levels (2.7-fold) are attenuated by SB-408124 (1.2-fold).