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CP-135807

CP-135807用途

CP-135807是一种口服活性和选择性5-HT1D激动剂(IC50＝3.1nM),牛)。CP-135807介导中枢精神活动,可用于抗抑郁研究[1][2]。

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CP-135807名称

[ CAS 号 ]:
151272-90-1

[ 英文名 ]:
CP-135807

[英文别名 ]:

CP 135,807

CP-135807生物活性

[ 描述 ]:

CP-135807是一种口服活性和选择性5-HT1D激动剂(IC50＝3.1nM),牛)。CP-135807介导中枢精神活动,可用于抗抑郁研究[1][2]。

[ 相关类别 ]:

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-HT1D Receptor:3.1 nM (IC50, rat)

5-HT1D Receptor:33 nM (IC50, bovine)

[体内研究]

鸽子被训练在一个固定比例的食物提供下啄一个键。CP-135807(0.1 mg/kg；肌肉注射; 单剂量) 则能够完全和剂量依赖地替代成年雄性卡诺鸽子的训练剂量[1]。

[参考文献]

[1]. Mansbach RS, et al. CP-135,807, a selective 5-HT1D agonist: effects in drug discrimination and punishment procedures in the pigeon. Psychopharmacology (Berl). 1996 Dec;128(3):313-9.

[2]. Macor J E, et al. Use of 2, 5-Dimethylpyrrole as an Amino-Protecting Group in an Efficient Synthesis of 5-Amino-3-[(N-methyl-pyrrolidin-2 (R)-yl) methyl] indole[J]. The Journal of Organic Chemistry, 1994, 59(24): 7496-7498.

CP-135807物理化学性质

[ 密度 ]:
1.343g/cm3

[ 沸点 ]:
548.7ºC at 760 mmHg

[ 分子式 ]:
C₁₉H₂₁N₅O₂

[ 分子量 ]:
351.40200

[ 闪点 ]:
285.6ºC

[ 精确质量 ]:
351.17000

[ PSA ]:
89.77000

[ LogP ]:
4.38550

[ 蒸汽压 ]:
4.33E-12mmHg at 25°C

[ 折射率 ]:
1.709

CP-135807MSDS

详细MSDS(安全技术说明书)

CP-135807安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ RTECS号 ]:
NL2412000

CP-135807文献

Combined administration of a 5-hydroxytryptamine (5-HT)1D antagonist and a 5-HT reuptake inhibitor synergistically increases 5-HT release in guinea pig hypothalamus in vivo.

J. Neurochem. 67(5) , 2204-7, (1996)

In vivo microdialysis in guinea pig hypothalamus was used to study the effect of serotonin [5-hydroxytryptamine (5-HT)] subtype 1D autoreceptor blockade on the increase in extracellular 5-HT levels pr...

In vitro characterization of AR-A000002, a novel 5-hydroxytryptamine(1B) autoreceptor antagonist.

Eur. J. Pharmacol. 499(1-2) , 67-75, (2004)

The in vitro pharmacological properties of AR-A000002 ((R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphthyl]-4-morpholinobenzamide), a novel 5-hydroxytryptamine (5-HT)(1B) receptor...

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