CP-135807

Names

[ Name ]:
CP-135807

[Synonym ]:
1H-Indol-5-amine,3-((1-methyl-2-pyrrolidinyl)methyl)-N-(3-nitro-2-pyridinyl)-,(R)
(R)-3-((1-Methyl-2-pyrrolidinyl)methyl)-N-(3-nitro-2-pyridinyl)-1H-indol-5-amine
CP 135,807
3-(N-Methylpyrrolidin-2-ylmethyl)-5-(3-nitropyrid-2-ylamino)-1H-indole

Biological Activity

[Description]:

CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1D Receptor:3.1 nM (IC50, rat)

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

[In Vivo]

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]。

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.343g/cm3

[ Boiling Point ]:
548.7ºC at 760 mmHg

[ Molecular Formula ]:
C₁₉H₂₁N₅O₂

[ Molecular Weight ]:
351.40200

[ Flash Point ]:
285.6ºC

[ Exact Mass ]:
351.17000

[ PSA ]:
89.77000

[ LogP ]:
4.38550

[ Vapour Pressure ]:
4.33E-12mmHg at 25°C

[ Index of Refraction ]:
1.709

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
NL2412000

Articles

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...