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SB408124

 
Catalog No.
B2163
OX(1)受体拮抗剂
组合的产品项目
规格价格库存 数量
5mg
¥ 454.00
现货
10mg
¥ 772.00
现货
25mg
¥ 1,727.00
现货
100mg
¥ 4,909.00
现货

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A

背景

SB408124是一种新型有效的非肽类食欲素-1(OX(1))受体拮抗剂,在细胞膜和全细胞中的Ki值分别为27 nM和57 nM.SB408124对OX1受体的选择性比人OX2受体高50倍[1].

在从大鼠大脑皮层中获得的原代星形细胞培养物中,使用食欲素A之前用SB408124预处理可显著降低食欲素A对毛喉素和基底诱导的cAMP生成的刺激活性[2].

在大鼠中,注射组胺(HA)或高盐水后,SB408124(30 μg/10 μl)与食欲素A共同给药可防止食欲素A诱导的对加压素(VP)浓度提高的减少[3].

参考文献:
[1] Langmead CJ1, Jerman JC, Brough SJ, Scott C, Porter RA, Herdon HJ. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141(2):340-6.
[2] Woldan-Tambor A1, Biegańska K, Wiktorowska-Owczarek A, Zawilska JB.  Activation of orexin/hypocretin type 1 receptors stimulates cAMP synthesis in primary cultures of rat astrocytes. Pharmacol Rep. 2011;63(3):717-23.
[3] Kis GK1, Molnár AH, Daruka L, Gardi J, Rákosi K, László F, László FA, Varga C. The osmotically and histamine-induced enhancement of the plasma vasopressin level is diminished by intracerebroventricularly administered orexin in rats. Pflugers Arch. 2012 Apr;463(4):531-6.

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt356.38
Cas No.288150-92-5
FormulaC19H18F2N4O
Solubilityinsoluble in H2O; ≥1.76 mg/mL in EtOH with gentle warming and ultrasonic; ≥35.4 mg/mL in DMSO with gentle warming
Chemical Name1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea
SDFDownload SDF
Canonical SMILESCC1=NC2=C(C=C(C=C2C(=C1)NC(=O)NC3=CC=C(C=C3)N(C)C)F)F
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