激动剂(含哌嗪基)

激动剂(含哌嗪基)用途

SNC80 (NIH 10815) 是一种有效的,高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂,Ki 为1.78 nM,IC50 为 2.73 nM。SNC80 还以 EC50 为 52.8 nM 来选择性激活 HEK293 细胞中的 μ-δ 异聚体。SNC80 具有抗伤害性,抗痛觉过敏和抗抑郁样作用,并可用于多种头痛症的研究。

点击显示

激动剂(含哌嗪基)名称

[ CAS 号 ]:
156727-74-1

[ 中文名 ]:
(+)-4-[(ΑR)-Α-((2S,5R)-4-烯丙基-2,5-二甲基-1-哌嗪基)-3-甲氧基苄基]-N,N-二乙基苯酰胺

[ 英文名 ]:
SNC80

[中文别名 ]:

[英文别名 ]:

SNC80
MFCD00672673
2-Pyridylethylamine dihydrochloride

激动剂(含哌嗪基)生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

信号通路 >> 神经信号通路 >> 阿片受体

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 2.73 nM (δ-opioid receptor), 5457 nM (μ-opioid receptor)[3] Ki: 1.78 nM (δ-opioid receptor), 881.5 nM (μ-opioid receptor) and 441.8 nM (κ-opioid receptor)[2]

[体外研究]

SNC80以52.8nm的EC50选择性激活HEK293细胞中的μ-δ异构体。SNC80在联合表达μ-和δ-阿片受体的细胞中显示出比单独表达δ-阿片受体或联合表达δ-和κ-阿片受体的细胞更大的活性[4]。

[体内研究]

SNC80(10mg/kg；腹腔注射；1次；C57BL6/J小鼠)治疗显著减轻了过量使用舒马曲坦引起的痛觉异常[1]。动物模型：雄性和雌性C57BL6/J小鼠(20-30g)注射舒马曲坦[1]剂量：10mg/kg给药：腹腔注射；1次结果：显著减轻痛觉过敏。

[参考文献]

[1]. Moye LS, et al. Delta opioid receptor agonists are effective for multiple types of headache disorders. Neuropharmacology. 2019 Apr;148:77-86.

[2]. Bilsky EJ, et al. SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist. J Pharmacol Exp Ther. 1995 Apr;273(1):359-66.

[3]. Calderon SN, et al. Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist. J Med Chem. 1994 Jul 8;37(14):2125-8.

[4]. Metcalf MD, et al. The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ opioid receptors. ACS Chem Neurosci. 2012 Jul 18;3(7):505-9.

[5]. Vicente-Sanchez A, et al. The delta opioid receptor tool box. Neuroscience. 2016 Dec 3;338:145-159.

[6]. Dripps IJ, et al. Role of signalling molecules in behaviours mediated by the δ opioid receptor agonist SNC80. Br J Pharmacol. 2018 Mar;175(6):891-901.

激动剂(含哌嗪基)物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
564.8±50.0 °C at 760 mmHg

[ 熔点 ]:
122-123ºC

[ 分子式 ]:
C₂₈H₃₉N₃O₂

[ 分子量 ]:
449.628

[ 闪点 ]:
295.4±30.1 °C

[ 精确质量 ]:
449.304230

[ PSA ]:
36.02000

[ LogP ]:
3.37

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.545

[ 储存条件 ]:
室温

激动剂(含哌嗪基)MSDS

激动剂(含哌嗪基)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

[ WGK德国 ]:
3

激动剂(含哌嗪基)合成路线

激动剂(含哌嗪基)上下游产品

激动剂(含哌嗪基)上游产品

激动剂(含哌嗪基)下游产品

激动剂(含哌嗪基)文献

PKA and ERK1/2 are involved in dopamine D₁ receptor-induced heterologous desensitization of the δ opioid receptor.

Life Sci. 92(23) , 1101-9, (2013)

Chronic administration of cocaine attenuates delta opioid receptor (DOPR) signaling in the striatum and the desensitization is mediated by the indirect actions of cocaine on dopamine D1 receptors (D1R...

Novel screening assay for the selective detection of G-protein-coupled receptor heteromer signaling.

J. Pharmacol. Exp. Ther. 344(1) , 179-88, (2013)

Drugs targeting G-protein-coupled receptors (GPCRs) make up more than 25% of all prescribed medicines. The ability of GPCRs to form heteromers with unique signaling properties suggests an entirely new...

Dual efficacy of delta opioid receptor-selective ligands for ethanol drinking and anxiety.

J. Pharmacol. Exp. Ther. 335(1) , 133-9, (2010)

Alcoholism and anxiety disorders have a huge impact on society and afflict 17.6 million and 40 million people in the United States, respectively. A strong comorbidity exists between alcoholism and anx...

更多文献