Naloxone (hydrochloride)
(Synonyms: 盐酸纳洛酮) 目录号 : GC11807
Naloxone (hydrochloride)是一种纯阿片受体拮抗剂。
Cas No.:357-08-4
Sample solution is provided at 25 µL, 10mM.
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Naloxone (hydrochloride) is a pure opioid receptor antagonist [1]. Naloxone can rapidly reverse opioid-induced symptoms such as respiratory depression and sedation [2]. Naloxone is widely used in emergency treatment for opioid overdose, particularly to treat respiratory failure and restore spontaneous breathing [3-4].
In MDAMB231 cells, Naloxone (1-100μM; 48h) inhibits the proliferation and enhances the apoptosis of cells [5]. In KF cells, Naloxone (120μM; 72h) inhibits the proliferation of cells [6].
In MCF-7 cells xenograft tumor mice model, Tumor growth was significantly inhibited in mice treated with Naloxone (0.36mg/kg, 0.7mg/kg; ip; 4weeks) [7]. In C57BL/6J mice, Naloxone (3mg/kg; ip; single injection) reverses the respiratory and analgesic effects of opioid agonists and induces withdrawal [8].
References:
[1]. Sawynok J, Pinsky C, LaBella F S. On the specificity of naloxone as an opiate antagonist[J]. Life Sciences, 1979, 25(19): 1621-1631.
[2]. Dahan A, Aarts L, Smith T W. Incidence, reversal, and prevention of opioid-induced respiratory depression[J]. Anesthesiology, 2010, 112(1): 226-238.
[3]. Britch S C, Walsh S L. Treatment of opioid overdose: current approaches and recent advances[J]. Psychopharmacology, 2022, 239(7): 2063-2081.
[4]. van Lemmen M, Florian J, Li Z, et al. Opioid overdose: limitations in naloxone reversal of respiratory depression and prevention of cardiac arrest[J]. Anesthesiology, 2023, 139(3): 342-353.
[5]. Bimonte S, Barbieri A, Cascella M, et al. The effects of naloxone on human breast cancer progression: in vitro and in vivo studies on MDA. MB231 cells[J]. OncoTargets and therapy, 2018: 185-191.
[6]. KIKUCHI Y, KITA T, MIYAUCHI M, et al. Effects of naloxone on human ovarian cancer cell growth in vitro and in vivo[J]. Japanese Journal of Cancer Research GANN, 1987, 78(5): 519-525.
[7]. Farooqui M, Geng Z H, Stephenson E J, et al. Naloxone acts as an antagonist of estrogen receptor activity in MCF-7 cells[J]. Molecular cancer therapeutics, 2006, 5(3): 611-620.
[8]. Lewanowitsch T, Miller J H, Irvine R J. Reversal of morphine, methadone and heroin induced effects in mice by naloxone methiodide[J]. Life sciences, 2006, 78(7): 682-688.
Naloxone (hydrochloride)是一种纯阿片受体拮抗剂 [1]。Naloxone可以快速逆转阿片类药物引起的呼吸抑制和镇静等症状 [2]。Naloxone广泛用于阿片类药物过量紧急治疗，尤其用于治疗呼吸衰竭和恢复自主呼吸 [3-4]。
在MDAMB231细胞中，Naloxone（1-100μM；48h）抑制细胞增殖并促进细胞凋亡 [5]。在KF细胞中，Naloxone（120μM；72h）抑制细胞增殖 [6]。
在MCF-7细胞异种移植瘤小鼠模型中，Naloxone（0.36mg/kg，0.7mg/kg； ip； 4weeks）治疗小鼠的肿瘤生长受到显著抑制 [7]。在C57BL/6J小鼠中，Naloxone（3mg/kg；ip；单次注射）可逆转阿片类激动剂的呼吸和镇痛作用，并诱导戒断反应 [8]。
| Cell experiment [1]: | |
Cell lines | MDAMB231 cells |
Preparation Method | The effect of the drug on cell proliferation was determined by using TACS (MTT) cell proliferation assay. The cells (2,000 per well) were incubated with or without Naloxone in triplicate in a 96-well plate and then incubated for 2, 4, and 6 days at 37℃. An MTT solution was added to each well and incubated for 2h at 37℃. An extraction buffer (20% SDS and 50% dimethylformamide) was added, and the cells were incubated overnight at 37℃. The absorbance of the cell suspension was measured at 570nm using a microplate reader. |
Reaction Conditions | 1-100μM; 48h |
Applications | Naloxone inhibits the proliferation and enhances the apoptosis of MDAMB231 cells. |
| Animal experiment [2]: | |
Animal models | MCF-7 cells xenograft tumor mice model |
Preparation Method | In the estrogen-dependent MCF-7 breast cancer xenograft model, six-week-old nude mice were implanted with slow-acting estradiol (E₂)-releasing microspheres to maintain estrogen levels. Subsequently, 5×106 MCF-7 cells were injected into the mammary fat pad. Following tumor inoculation, mice received daily intraperitoneal injections of Naloxone (0.36mg/kg once daily for the first two weeks, then 0.7mg/kg for the next two weeks) and were observed until the end of the experiment. |
Dosage form | 0.36mg/kg, 0.7mg/kg; ip; 4weeks |
Applications | Tumor growth was significantly inhibited in mice treated with Naloxone. |
References: | |
| Cas No. | 357-08-4 | SDF | |
| 别名 | 盐酸纳洛酮 | ||
| 化学名 | (4R,4aS,7aR,12bS)-3-allyl-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one hydrochloride | ||
| Canonical SMILES | O[C@@]12[C@@]3([C@]([H])(C(CC2)=O)O4)CCN([C@@H]1CC5=CC=C(O)C4=C35)CC=C.Cl | ||
| 分子式 | C19H22ClNO4 | 分子量 | 363.84 |
| 溶解度 | ≥ 18.19mg/mL in DMSO | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7485 mL | 13.7423 mL | 27.4846 mL |
| 5 mM | 0.5497 mL | 2.7485 mL | 5.4969 mL |
| 10 mM | 0.2748 mL | 1.3742 mL | 2.7485 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet