Naltrexone 

Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight^{[1][2][3][4][5]}.

Naltrexone (1-100 μM; 48-120 h) inhibited proliferation of SKOV-3, MDA-MB-231, SK-N-MC, OVCAR-3, MIA PaCa-2, SCC-1, and HCT-116 cancer cells via intermittent or short-term treatment, while continuous treatment stimulated proliferation^[3].
Naltrexone (1.0 mg/mL; 24-72 h) inhibited proliferation of SW480 and HCT116 colon cancer cells in a time-dependent manner, with maximum inhibition at 72 h^[3].
Naltrexone (1 μM) increases the activity of mouse hypothalamic arcuate POMC-EGFP cells in vitro, and this effect is amplified when combined with Bupropion^[5].

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

Naltrexone (0.1-10 mg/kg; i.p.; 1, 3, 7 times per week) at low-dose administration extends tumorigenesis latency in a frequency-dependent manner, whereas high-dose treatment shortens tumorigenesis latency in mice bearing human squamous cell carcinoma SCC-1^[3].
Naltrexone (0.1 mg/kg; i.p.; daily administration; for 40 consecutive days) reduces the number and weight of tumor nodules in mice bearing SKOV-3 human epithelial ovarian cancer^[3].
Naltrexone (1-75 mg/kg; administered via dietary supplementation or injection; dosing frequency of twice weekly or twice daily; treatment duration of 25 days) reduces the tumor volume and diameter in DMBA (HY-W011845)-induced breast cancer rats, and a higher dose of the injection route results in a greater reduction in tumor diameter^[3].
Naltrexone (0.1-10 mg/kg; intravenous injection; once daily; for 75 consecutive days) at low-dose administration extend the survival time of mice in the S20Y mouse neuroblastoma model, while high doses increase tumor diameter, shorten the latency period, and reduce survival time in this mouse model^[3].
Naltrexone (0.1 mg/kg; intravenous injection; once daily; for 50 consecutive days) reduces tumor incidence and prolongs the latency period in mice bearing HT-29 human colon cancer^[3].
Naltrexone reduces food intake in diet-induced obesity (DIO) mice and fasted lean mice, and exerts a synergistic effect when combined with Bupropion^[5].

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

341.40

C₂₀H₂₃NO₄

16590-41-3

Solid

White to off-white

OC1=CC=C2C3=C1O[C@](C(CC4)=O)([H])[C@@]3(CCN5CC6CC6)[C@]4(O)[C@@]5([H])C2

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Lee B, et al. The uses of naltrexone in dermatologic conditions. J Am Acad Dermatol. 2019;80(6):1746-1752.  [Content Brief]

  [2]. Younger J, et al. The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain. Clin Rheumatol. 2014;33(4):451-459.  [Content Brief]

  [3]. Liubchenko K, et al. Naltrexone's Impact on Cancer Progression and Mortality: A Systematic Review of Studies in Humans, Animal Models, and Cell Cultures. Adv Ther. 2021;38(2):904-924.  [Content Brief]

  [4]. Lobmaier PP, et al. Naltrexone depot formulations for opioid and alcohol dependence: a systematic review. CNS Neurosci Ther. 2011;17(6):629-636.  [Content Brief]

  [5]. Billes SK, et al. Naltrexone/bupropion for obesity: an investigational combination pharmacotherapy for weight loss. Pharmacol Res. 2014;84:1-11.  [Content Brief]