盐酸扎利罗登

盐酸扎利罗登用途

Xaliproden hydrochloride (SR57746A) 是一种有效、选择性和具有口服活性的 5-HT1A 受体激动剂,对大鼠海马中的 5-HT1A 特异性结合位点表现出高亲和力 (IC50=3 nM)。Xaliproden hydrochloride 也是一种选择性的多巴胺 D2 受体拮抗剂,具有中等亲和力 (IC50=0.1-1 μM)。Xaliproden hydrochloride 具有抗抑郁作用和抗焦虑作用,并且具有研究神经退行性疾病的潜力。

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盐酸扎利罗登名称

[ CAS 号 ]:
90494-79-4

[ 中文名 ]:
盐酸扎利罗登

[ 英文名 ]:
Xaliproden hydrochloride

[中文别名 ]:

[英文别名 ]:

Xaliproden hydrochloride

盐酸扎利罗登生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT1A Receptor:3 nM (IC50)

D2 Receptor:0.1-1 μM (IC50)

[参考文献]

[1]. Cervo L, et, al. Potential antidepressant properties of SR 57746A, a novel compound with selectivity and high affinity for 5-HT1A receptors. Eur J Pharmacol. 1994 Feb 21; 253(1-2): 139-47.

[2]. Simiand J, et, al. Neuropsychopharmacological profile in rodents of SR 57746A, a new, potent 5-HT1A receptor agonist. Fundam Clin Pharmacol. 1993;7(8):413-27.

[3]. Fournier J, et, al. Protective effects of SR 57746A in central and peripheral models of neurodegenerative disorders in rodents and primates. Neuroscience. 1993 Aug; 55(3): 629-41.

盐酸扎利罗登物理化学性质

[ 沸点 ]:
487.8ºC at 760mmHg

[ 分子式 ]:
C₂₄H₂₃ClF₃N

[ 分子量 ]:
417.89400

[ 闪点 ]:
248.8ºC

[ 精确质量 ]:
417.14700

[ PSA ]:
3.24000

[ LogP ]:
6.93030

[ 外观性状 ]:
固体

[ 储存条件 ]:
2-8°C，密封，干燥

盐酸扎利罗登MSDS

详细MSDS(安全技术说明书)

盐酸扎利罗登安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

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

[ RTECS号 ]:
UT8405666

盐酸扎利罗登文献

5-HT1A receptors are involved in the effects of xaliproden on G-protein activation, neurotransmitter release and nociception.

Br. J. Pharmacol. 158(1) , 232-42, (2009)

Xaliproden (SR57746A) is a 5-HT(1A) receptor agonist and neurotrophic agent that reduces oxaliplatin-mediated neuropathy in clinical trials. The present study investigated its profile on in vitro tran...

Magnetic resonance imaging of the neuroprotective effect of xaliproden in rats.

Invest. Radiol. 37(6) , 321-7, (2002)

The neurotrophic effect of Xaliproden has been followed using sequential cerebral magnetic resonance imaging (MRI) in rats with vincristine-induced brain lesion as a model of Alzheimer disease.Ninetee...

The neuroprotective agent SR 57746A abrogates experimental autoimmune encephalomyelitis and impairs associated blood-brain barrier disruption: implications for multiple sclerosis treatment.

Proc. Natl. Acad. Sci. U. S. A. 96(22) , 12855-9, (1999)

Experimental autoimmune encephalomyelitis (EAE) is a T cell autoimmune disorder that is a widely used animal model for multiple sclerosis (MS) and, as in MS, clinical signs of EAE are associated with ...

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