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)
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SB-408124 Hydrochloride
CAS number:1431697-90-3 molecular formula:C19H19ClF2N4O
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| Chinese alias | SB-408124 盐酸盐 | ||
| English alias | N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]urea hydrochloride | F84881 | MS-26581 | SB-408124 HCl | SB-408124 Hydrochloride | AKOS030526528 | SB-408124 (Hydrochloride) | 1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)ph | ||
| CAS number | 1431697-90-3 | molecular formula | C19H19ClF2N4O |
| molecular weight | 392.83 g/mol | Exact mass | ≥98% |
| PSA | 57.300 Ų | logp | - |
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