- 英文名称
- SNC 80
- 分子式
- C28H39N3O2
- 分子量
- 449.63
- 中文别名
- 4-[(R)-[(2S,5R)-2,5-二甲基-4-(2-丙烯-1-基)-1-哌嗪基](3-甲氧基苯基)甲基]-N,N-二乙基苯甲酰胺; 化合物SNC80; SNC80,Δ阿片受体激动剂; SNC80,DELTA OPIOID RECEPTOR激动剂; 4-[(R)-[(2S,5R)-2,5-Dimethyl-4-(2-propen-1-yl)-1-piperazinyl](3-methoxyphenyl)methyl]-N,N-diethylbenzamide; (+)-4-[(Ar)-alpha-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)-3; NIH 10815; (+)-4-[(AR)-A-((2S,5R)-4-ALLYL-2,5-DIMETHYL-1-PIPERAZINYL)-3-METHOXYBENZYL]-N,N-DIETHYLBENZAM; (+)-4-[(AR)-A-((2S,5R)-4-ALLYL-2,5-DIMETHYL-1-PIPERAZINYL)-3-METHOXYBENZYL]-N,N-DIETHYLBENZAMIDE; (+)-4-[(AR)-ALPHA-((2S,5R)-4-ALLYL-2,5-DIMETHYL-1-PIPERAZINYL)-3-METHOXYBENZYL]-N,N-DIETHYLBENZAMIDE; (+)-4-[(αr)-α-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-n,n-diethylbenzamide; 4-[(R)-[(2S,5R)-2,5-dimethyl-4-prop-2-enylpiperazin-1-yl]-(3-methoxyphenyl)methyl]-N,N-diethylbenzamide; 4-[(R)-[(2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl](3-methoxyphenyl)methyl]-N,N-diethylbenzamide; SNC80; 4-[(R)-[(2S,5R)-4-Allyl-2,5-dimethylpiperazin-1-yl](3-methoxyphenyl)methyl]-N,N-diethylbenzamide
- 用途
- - 生物活性
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。
- 靶点
IC50: 2.73 nM (δ-opioid receptor), 5457 nM (μ-opioid receptor)
Ki: 1.78 nM (δ-opioid receptor), 881.5 nM (μ-opioid receptor) and 441.8 nM (κ-opioid receptor)
- 体外研究
SNC80 selectively activates μ-δ heteromer in HEK293 cells with an EC
50
of 52.8 nM. SNC80 exhibits substantially greater activity in cells coexpressing μ- and δ-opioid receptors than in cells either singly expressing δ-opioid receptors or coexpressing δ- and κ-opioid receptors.
- 体内研究
SNC80 (10 mg/kg; intraperitoneal injection; once; C57BL6/J mice) treatment significantly attenuated this allodynia caused by overuse of Sumatriptan.
Animal Model:
Male and female C57BL6/J mice (20-30g) injected with Sumatriptan
Dosage:
10 mg/kg
Administration:
Intraperitoneal injection; once
Result:
Significantly attenuated allodynia.
- A highly selective and potent non-peptide Δ9-agonist, 2000-fold selective over u-receptors.
