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SB-408124

SB-408124用途

SB408124是非肽类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。

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SB-408124名称

[ CAS 号 ]:
288150-92-5

[ 中文名 ]:
N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素

[ 英文名 ]:
SB408124

[中文别名 ]:

[英文别名 ]:

MFCD06411575
S1545_Selleck
SB-408,124
SB-408124

SB-408124生物活性

[ 描述 ]:

SB408124是非肽类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。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 食欲素受体(OX受体)

研究领域 >> 神经疾病

[参考文献]

[1]. Morairty SR, et al. Dual hypocretin receptor antagonism is more effective for sleep promotion than antagonism of either receptor alone.PLoS One. 2012;7(7):e39131. Epub 2012 Jul 2.

[2]. Melis MR, et al. Neuroendocrine regulatory peptide-1 and neuroendocrine regulatory peptide-2 influence differentially feeding and penile erection in male rats: sites of action in the brain.Regul Pept. 2012 Aug 20;177(1-3):46-52. Epub 2012 May 2.

[3]. Assisi L, et al. Expression and role of receptor 1 for orexins in seminiferous tubules of rat testis.Cell Tissue Res. 2012 Jun;348(3):601-7. Epub 2012 Mar 28.

[4]. Kis GK, et al. 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. Epub 2012 Feb 16.

[5]. Langmead et al (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br.J.Pharmacol. 141 340.

[相关活性小分子]

SB-408124物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
430.3±45.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₁₈F₂N₄O

[ 分子量 ]:
356.369

[ 闪点 ]:
214.0±28.7 °C

[ 精确质量 ]:
356.144867

[ PSA ]:
57.26000

[ LogP ]:
4.53

[ 外观性状 ]:
solid | olive-green

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.697

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ~24 mg/mL

SB-408124安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

SB-408124文献

A major role for perifornical orexin neurons in the control of glucose metabolism in rats.

Diabetes 58(9) , 1998-2005, (2009)

The hypothalamic neuropeptide orexin influences (feeding) behavior as well as energy metabolism. Administration of exogenous orexin-A into the brain has been shown to increase both food intake and blo...

Hypocretin/orexin type 1 receptor in brain: role in cardiovascular control and the neuroendocrine response to immobilization stress.

Am. J. Physiol. Regul. Integr. Comp. Physiol. 292(1) , R382-7, (2007)

Hypocretin/orexin acts pharmacologically in the hypothalamus to stimulate stress hormone secretion at least in part by an action in the hypothalamic paraventricular nucleus, where the peptide's recept...

Modulation of respiratory activity by hypocretin-1 (orexin A) in situ and in vitro.

Adv. Exp. Med. Biol. 669 , 109-13, (2010)

Release of hypocretins (orexins) by neurons in the lateral hypothalamus is an important contributor to arousal state, thermoregulation, feeding behavior, and has recently been proposed to play a role ...

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