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N-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-N-2-吡啶基环己烷甲酰胺

用途

WAY-100635马来酸盐是5-HT受体拮抗剂,IC50为0.95nM。

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名称

[ CAS 号 ]:
634908-75-1

[ 中文名 ]:
N-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-N-2-吡啶基环己烷甲酰胺

[ 英文名 ]:
WAY-100635 (maleate salt)

[英文别名 ]:

WAY-100635
WAY100635 maleate salt
WAY-100635 (maleate salt)

生物活性

[ 描述 ]:

WAY-100635马来酸盐是5-HT受体拮抗剂,IC50为0.95nM。

[ 相关类别 ]:

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

研究领域 >> 神经疾病

[参考文献]

[1]. Choi JY, Kim CH, Jeon TJ, Kim BS, Yi CH, Woo KS, Seo YB, Han SJ, Kim KM, Yi DI, Lee M, Kim DG, Kim JY, Lee KC, Choi TH, An G, Ryu YH.Effective microPET imaging of brain 5-HT(1A) receptors in rats with [(18) F]MeFWAY by suppression of radioligand defluorin

[2]. Mannucci C, Navarra M, Calzavara E, Caputi AP, Calapai G.Serotonin involvement in Rhodiola rosea attenuation of nicotine withdrawal signs in rats.Phytomedicine. 2012 Aug 23.

[3]. Katsidoni V, Anagnostou I, Panagis G.Cannabidiol inhibits the reward-facilitating effect of morphine: involvement of 5-HT(1A) receptors in the dorsal raphe nucleus.Addict Biol. 2012 Aug 2.

[4]. Paquette MA, Martinez AA, Macheda T, Meshul CK, Johnson SW, Berger SP, Giuffrida A.Anti-dyskinetic mechanisms of amantadine and dextromethorphan in the 6-OHDA rat model of Parkinson's disease: role of NMDA vs. 5-HT1A receptors.Eur J Neurosci. 2012 Aug 3.

[5]. Al Hussainy, Rana; Design, Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of Bridgehead Iodinated Analogues of N-{2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as Potential SPECT Ligands for

[相关活性小分子]

物理化学性质

[ 沸点 ]:
594.8ºC at 760 mmHg

[ 分子式 ]:
C₂₉H₃₈N₄O₆

[ 分子量 ]:
538.635

[ 闪点 ]:
313.5ºC

[ 精确质量 ]:
538.279114

[ PSA ]:
123.51000

[ LogP ]:
3.54040

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
-20°C

MSDS

详细MSDS(安全技术说明书)

安全信息

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

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

文献

LSD but not lisuride disrupts prepulse inhibition in rats by activating the 5-HT(2A) receptor.

Psychopharmacology 208(2) , 179-89, (2010)

Compounds that activate the 5-HT(2A) receptor, such as lysergic acid diethylamide (LSD), act as hallucinogens in humans. One notable exception is the LSD congener lisuride, which does not have halluci...

The selective 5-HT1A antagonist radioligand [3H]WAY 100635 labels both G-protein-coupled and free 5-HT1A receptors in rat brain membranes.

Eur. J. Pharmacol. 288 , 173, (1995)

The tritiated derivative of the novel silent 5-HT1A receptor antagonist WAY 100635 [N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl) cyclohexane carboxamide] was tested as a potential ra...

Electrophysiological, biochemical, neurohormonal and behavioural studies with WAY-100635, a potent, selective and silent 5-HT1A receptor antagonist.

Behav. Brain Res. 73 , 337, (1996)

Although considerable progress has been made in characterising the 5-HT1A receptor using agonists, partial agonists or non-selective antagonists, further studies of 5-HT1A receptor function have been ...

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