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/ 阿片受体 / Nociceptin/孤菲肽

Nociceptin/孤菲肽 {[allProObj[0].p_purity_real_show]}

货号：A210766 同义名： Orphanin FQ

Nociceptin是一种17氨基酸的神经肽，是ORL1（类似阿片受体1）的内源性配体。

Nociceptin/孤菲肽 化学结构 CAS号：170713-75-4
Nociceptin/孤菲肽 化学结构
CAS号：170713-75-4
Nociceptin/孤菲肽 3D分子结构
CAS号：170713-75-4
Nociceptin/孤菲肽 化学结构 CAS号：170713-75-4
Nociceptin/孤菲肽 3D分子结构 CAS号：170713-75-4
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Nociceptin/孤菲肽 纯度/质量文件 产品仅供科研

货号：A210766 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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产品名称 Opioid receptor ↓ ORL1 ↓ μ-opioid receptor ↓ 其他靶点 纯度
Racecadotril ✔ 98%
JTC-801 ++

Opioid receptor-like1 (ORL1), IC50: 94 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Nociceptin/孤菲肽 生物活性

描述 Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic. Nociceptin (1 μg/mL) significantly prevents LPS (10 ng/mL)-stimulated cell migration whereas it is ineffective when added alone. Nociceptin (1 nM-10 μM) elicits a concentration-dependent blockade of LPS-mediated cell migration, with a maximal effect at 1 and 10 μM. Nociceptin counteracts LPS-induced elevation of IL-1β mRNA levels. Nociceptin (1 μM) and NNC 55-0396 induce apoptotic cell death in U87 cells. Nociceptin (1 μM) counteracts LPS-induced [Ca2+]i increase in U87 cells via β-arrestin 2. Nociceptin counteracts the LPS-induced phosphorylation of PKC and ERK in U87 cells. Nociceptin inhibits the LPS-mediated transcriptional activation of NF-kB and AP-1 reporter genes[1]. The i.v. administration of nociceptin (10-100 nmol/kg) inhibits the micturition reflex in a naloxone-resistant manner. Intrathecal nociceptin (10 nmol/rat) produces urodynamic modifications similar to those induced by the i.v. administration. Intracerebroventricular (i.c.v.) administration of nociceptin (0.3-1 nmol/rat) also inhibited the micturition reflex in a naloxone-resistant manner suggesting a direct effect on supraspinal sites controlling the micturition. The application of nociceptin (5-50 nmol/rat) onto the bladder serosa when the intravesical volume was subthreshold for the triggering of the micturition reflex, activated the reflex in a dose-dependent manner; the same treatment produced a biphasic effect on the ongoing reflex[2]. Injection of nociceptin into mice stimulated Rec8 phosphorylation and meiotic chromosome dynamics in testes, whereas injection of nocistatin, a specific inhibitor for nociceptin, abolished them[3].

Nociceptin/孤菲肽 细胞实验

Cell Line
Concentration Treated Time Description References
Neurons in CeA slices 500 nM 10 minutes To investigate the effect of Nociceptin on GABAergic transmission in CeA neurons, results showed that Nociceptin significantly decreased sIPSC frequency in oxycodone-dependent HA rats but had less effect on LA and naive rats. Proc Natl Acad Sci U S A. 2020 Jan 28;117(4):2140-2148

Nociceptin/孤菲肽 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Rats with high (HA) and low (LA) addiction-like behaviors Bilateral CeA injections 1 μg/0.5 μL/site Single injection To investigate the effect of Nociceptin on oxycodone self-administration, results showed that Nociceptin selectively reduced oxycodone intake in HA rats but was ineffective in LA rats. Proc Natl Acad Sci U S A. 2020 Jan 28;117(4):2140-2148
Guinea-pigs Capsaicin-induced cough model Intracerebroventricular (i.c.v.) and intravenous (i.v.) 10, 30, 90 μg (i.c.v.); 0.3, 1.0, 3.0 mg/kg (i.v.) Single dose, 15 minutes before capsaicin challenge To evaluate the inhibitory effect of Nociceptin on capsaicin-induced cough. Results showed that both i.c.v. and i.v. administration dose-dependently inhibited cough, and the effect of i.c.v. administration (90 μg) was blocked by ORL1 receptor antagonists but not affected by the opioid receptor antagonist naltrexone. Br J Pharmacol. 2001 Mar;132(6):1175-8
Guinea pigs HCl-induced airway microvascular leakage model Intravenous injection 3–30 μg/kg Single dose, administered 1 min before Evans blue dye To investigate the inhibitory effect of Nociceptin on HCl-induced airway microvascular leakage, showing that Nociceptin inhibited leakage in a dose-dependent manner, with maximal inhibition at 30 μg/kg. Br J Pharmacol. 2004 Mar;141(6):1077-83

Nociceptin/孤菲肽 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03193398 Major Depressive Disorder Phase 2 Active, not recruiting December 2018 United States, California ... 展开 >> United States Cerritos, California, United States, 90703 United States Garden Grove, California, United States, 92845 United States, Florida United States, Florida Jacksonville, Florida, United States, 32256 United States Lauderhill, Florida, United States, 33319 United States, Florida Orlando, Florida, United States, 32801 United States, Illinois United States Libertyville, Illinois, United States, 60048 United States, New York United States Rochester, New York, United States, 14618 United States, Tennessee United States Memphis, Tennessee, United States, 38119 收起 <<
NCT03302416 Healthy Early Phase 1 Recruiting June 1, 2019 United States, Pennsylvania ... 展开 >> University of Pittsburgh Recruiting Pittsburgh, Pennsylvania, United States, 15213 收起 <<
NCT00173225 - Unknown - Taiwan ... 展开 >> Ping-Hung Kuo Recruiting Taipei, Taiwan, 100 Contact: Ping-Hung Kuo, MD    886-2-23123456 ext 3075    kph@ntumc.org    Principal Investigator: Ping-Hung Kuo, MD 收起 <<

Nociceptin/孤菲肽 参考文献

[1]Bedini A, Baiula M, Vincelli G, Formaggio F, Lombardi S, Caprini M, Spampinato S. Nociceptin/orphanin FQ antagonizes lipopolysaccharide-stimulated proliferation, migration and inflammatory signaling in human glioblastoma U87 cells. Biochem Pharmacol. 2017 Sep 15;140:89-104

[2]Lecci A, Giuliani S, Meini S, Maggi CA. Nociceptin and the micturition reflex. Peptides. 2000 Jul;21(7):1007-21

[3]Eto K. Nociceptin and meiosis during spermatogenesis in postnatal testes. Vitam Horm. 2015;97:167-86

Nociceptin/孤菲肽 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.55mL

0.11mL

0.06mL

2.76mL

0.55mL

0.28mL

5.53mL

1.11mL

0.55mL

Nociceptin/孤菲肽 技术信息

CAS号170713-75-4
分子式C79H129N27O22
分子量 1809.04
SMILES Code NC(CC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@H](CC1=CC=CC=C1)NC(CNC(CNC([C@H](CC2=CC=CC=C2)N)=O)=O)=O)=O)[C@@H](C)O)=O)=O)C)=O)CCCNC(N)=N)=O)CCCCN)=O)CO)=O)C)=O)CCCNC(N)=N)=O)CCCCN)=O)CC(C)C)=O)C)=O)CC(N)=O)=O)C(O)=O)=O
MDL No. MFCD05861378
别名 Orphanin FQ
运输蓝冰
InChI Key PULGYDLMFSFVBL-SMFNREODSA-N
Pubchem ID 16131448
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 50 mg/mL(27.64 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(27.64 mM)

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Nociceptin | 170713-75-4 | Orphanin FQ | Opioid Receptor | GPCR/G Protein | Neuronal Signaling | Opioid Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Nociceptin/孤菲肽 纯度/质量文件 | Nociceptin/孤菲肽 亚型比较 | Nociceptin/孤菲肽 生物活性 | Nociceptin/孤菲肽 临床数据 | Nociceptin/孤菲肽 参考文献 | Nociceptin/孤菲肽 实验方案 | Nociceptin/孤菲肽 技术信息

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