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[6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮

用途

AM630 是一种选择性的 CB₂ 拮抗剂，K_i 值为 31.2 nM，对其选择性是对 CB₁ 受体的 165 倍。

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名称

[ CAS 号 ]:
164178-33-0

[ 中文名 ]:
[6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮

[ 英文名 ]:
AM630

[中文别名 ]:

[英文别名 ]:

AM-630
AM630

生物活性

[ 描述 ]:

6-Iodopravadoline (AM630) 是一种选择性的 CB2 拮抗剂,Ki 值为 31.2 nM,对其选择性是对 CB1 受体的 165 倍。

[ 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 >> 大麻素受体

[ 靶点 ]

Ki: 31.2 nM (CB2)

[参考文献]

[1]. Garcia-Gutierrez, Maria S., et al. Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABAA receptors. British Journal of Pharmacology (2012), 165(4), 951-964.

[2]. Patil, Mayur., et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology (2011), 61(4), 778-788.

[3]. Geng, D. C., et al. Inhibition of titanium particle-induced inflammatory osteolysis through inactivation of cannabinoid receptor 2 by AM630. Journal of Biomedical Materials Research, Part A (2010), 95A(1), 321-326.

[4]. Mukherjee, Sutapa., et al. Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors. European Journal of Pharmacology (2004), 505(1-3), 1-9.

[5]. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814.

物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
605.9±55.0 °C at 760 mmHg

[ 分子式 ]:
C₂₃H₂₅IN₂O₃

[ 分子量 ]:
504.361

[ 闪点 ]:
320.3±31.5 °C

[ 精确质量 ]:
504.090973

[ PSA ]:
43.70000

[ LogP ]:
4.65

[ 外观性状 ]:
灰白色固体

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.647

[ 储存条件 ]:
2-8°C

安全信息

[ 符号 ]:

GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H410

[ 警示性声明 ]:
P273-P501

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

文献

Lack of presynaptic interaction between glucocorticoid and CB1 cannabinoid receptors in GABA- and glutamatergic terminals in the frontal cortex of laboratory rodents.

Neurochem. Int. 90 , 72-84, (2015)

Corticosteroid and endocannabinoid actions converge on prefrontocortical circuits associated with neuropsychiatric illnesses. Corticosteroids can also modulate forebrain synapses by using endocannabin...

Colon carcinogenesis is inhibited by the TRPM8 antagonist cannabigerol, a Cannabis-derived non-psychotropic cannabinoid.

Carcinogenesis 35(12) , 2787-97, (2014)

Cannabigerol (CBG) is a safe non-psychotropic Cannabis-derived cannabinoid (CB), which interacts with specific targets involved in carcinogenesis. Specifically, CBG potently blocks transient receptor ...

A Sativex(®) -like combination of phytocannabinoids as a disease-modifying therapy in a viral model of multiple sclerosis.

Br. J. Pharmacol. 172 , 3579-95, (2015)

Sativex(®) is an oromucosal spray, containing equivalent amounts of Δ(9) -tetrahydrocannabinol (Δ(9) -THC) and cannabidiol (CBD)-botanical drug substance (BDS), which has been approved for the treatme...

更多文献

[6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮

用途

名称

生物活性

物理化学性质

安全信息

文献

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