156727-74-1 (+)-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

WGK Germany:3 存储类别:11 - 可燃固体

• 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.

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