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]。