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CAS No. : 1431697-90-3
MCE 国际站:SB-408124 Hydrochloride
产品活性:SB-408124 Hydrochloride 是一种选择性的非肽类 OX1 受体拮抗剂,在全细胞和细胞膜分析中 Ki 为 57 nM 和 27 nM,比对 OX2 受体的抑制性高 50 倍。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Orexin Receptor (OX 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 vasopressin (AVP) mRNA levels (2.7-fold) are attenuated by SB-408124 (1.2-fold).
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.
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