2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Sunobinop TFA

Sunobinop TFA  (Synonyms: S 117957 TFA; IMB 115 TFA)

目录号: HY-139583A
一键复制产品信息 纯度: 98.26%
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Sunobinop (S 117957) TFA 是一种口服有效和可透过血脑屏障的选择性人孤啡肽/孤啡肽 FQ 受体 (NOP) 部分激动剂，对人源靶点表现出高亲和力 (Ki=3.3 nM；EC50=4.03 nM；Emax=47.8%)，同时不激活 μ 和 κ 阿片受体。Sunobinop TFA 通过激活 NOP 受体显著减少大鼠觉醒时间并增加非快速眼动睡眠，且在有效剂量下未对学习、记忆、奖赏、呼吸或肠道功能产生显著副作用。Sunobinop TFA 在特定信号通路 (如 β-Arrestin 2 招募) 中显示出竞争性拮抗剂特性。Sunobinop TFA 可用于研究失眠症、中重度酒精使用障碍及膀胱过度活动症所致尿失禁。

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Sunobinop TFA

Sunobinop TFA Chemical Structure

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1 mg ￥3350
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Customer Review

Other Forms of Sunobinop TFA:

Sunobinop TFA 相关抗体

Top Publications Citing Use of Products

查看 Opioid Receptor 亚型特异性产品:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sunobinop (S 117957) TFA is an orally active and blood-brain barrier-permeable selective partial agonist of the human nociceptin/orphanin FQ receptor (NOP), which exhibits high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%) without activating μ and κ opioid receptors. Sunobinop TFA significantly reduces wakefulness time and increases non-rapid eye movement sleep in rats by activating NOP receptors, and produces no significant side effects on learning, memory, reward, respiration or intestinal function at effective doses. Sunobinop TFA displays competitive antagonist properties in specific signaling pathways, such as β-arrestin 2 recruitment. With these unique pharmacological properties, Sunobinop TFA can be used to investigate insomnia, moderate-to-severe alcohol use disorder, and urinary incontinence caused by overactive bladder[1][2].

IC50 & Target[1]

NOP Receptor/ORL1

3.3 nM (Ki)

体外研究
(In Vitro)

Sunobinop (1 pM-1 μM) TFA 是钙动员实验中人源 NOP 受体的中等效力部分激动剂，且在经典阿片受体上无活性，显示出对 NOP 受体的高选择性[2]。
Sunobinop (10 pM-10 μM; 1 h 预孵育) TFA 在 cAMP 抑制实验中作为人 NOP 受体的中等效力部分激动剂，可降低福斯高林刺激的 cAMP 水平，效力约为 N/OFQ 最大效力的 72%[2]。
Sunobinop (10 pM-10 μM) TFA 在表达 NOP 受体的 HEK293 细胞生物阻抗分析中可作为一种低效、中等效力的部分激动剂，且在与 N/OFQ 共孵育时发挥竞争性拮抗剂的作用[2]。
Sunobinop TFA 在各项 NOP 实验中的人源 pEC50 值分别为 7.99、7.62、7.22 和 8.07[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Sunobinop TFA 相关抗体:
体内研究
(In Vivo)

Sunobinop (30-300 mg/kg; p.o.; 单次) TFA 可通过激活 NOP 受体显著减少 WT 大鼠的觉醒时间并增加非快速眼动 (non-REM) 睡眠，且在超治疗剂量下对认知、奖赏、呼吸或胃肠功能无不良影响[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wild-type rat with Insomnia (WT); NOP-knockout (NOP-KO)[1]
Dosage: 30 mg/kg; 300 mg/kg
Administration: p.o.; single dose
Result: Decreased wakefulness, increased non-REM sleep at 30 mg/kg and 300 mg/kg.
Caused no significant change in REM sleep at 300 mg/kg compared to controls.
Near-abolished the significant non-REM sleep increase observed in WT rats at 300 mg/kg when administered to NOP-KO rats.
Showed no statistically significant treatment-related changes in learning and memory, reward, respiration, or intestinal transit at supratherapeutic doses.
分子量

549.58

Formula

C28H34F3N3O5
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

纯度 & 产品资料
参考文献

Sunobinop TFA 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SunobinopS 117957IMB 115S117957S-117957IMB115IMB-115Opioid Receptoroveractive bladderratsHEK293 cellmouse vas deferensμ receptorsnociceptin/orphanin FQ receptor (NOP)insomnia disorderδ receptorsκ receptorsalcohol use disordersInhibitorinhibitorinhibit

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