Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University, 815 Hwarangro, Nowon-gu, Seoul, 01795, Republic of Korea.
Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University, 815 Hwarangro, Nowon-gu, Seoul, 01795, Republic of Korea; Department of Biological Sciences, University of Texas Dallas, Richardson, TX 75080, United States.
Neurochem Int. 2019 Jan;122:1-7. doi: 10.1016/j.neuint.2018.10.020. Epub 2018 Oct 24.
Methoxetamine (MXE) is an N-methyl-D-aspartate (NMDA) receptor antagonist that is chemically and pharmacologically similar to other dissociative substances, such as ketamine and phencyclidine. There are reports on the misuse of MXE, which sometimes resulted in adverse consequences and death. Studies have also shown that MXE has abuse liability and stimulates dopamine neurotransmission in the mesolimbic reward pathway in the brain. These findings have contributed to the negative impression on MXE. However, recent preclinical studies have identified the antidepressant properties of MXE, which are attributed to its ability to affect the glutamatergic and serotonergic systems. MXE is also reported to have analgesic effects. These findings show some of the "redeeming qualities" of MXE and indicate its possible therapeutic uses. In this paper, we have reviewed the findings that provide insights into the adverse and potential therapeutic effects of MXE. We compiled studies on the toxicity, psychotomimetic effects, and abuse liability of MXE, as well as its promising antidepressant and analgesic properties. We also have discussed the mechanism of action that might mediate the somewhat paradoxical effects observed. Importantly, this review provides valuable information on MXE for future research and will enable a better understanding of its psychopharmacological properties and the mechanisms responsible for its unique effects.
甲氧基苯己酮（MXE）是一种 N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，在化学结构和药理学特性上与其他致分离物质（如氯胺酮和苯环利定）相似。有关于 MXE 被滥用的报告，其中一些报告导致了不良后果甚至死亡。研究还表明，MXE 具有滥用潜力，并刺激大脑中中脑边缘奖赏通路中的多巴胺神经递质传递。这些发现导致了对 MXE 的负面印象。然而，最近的临床前研究已经确定了 MXE 的抗抑郁特性，这归因于其影响谷氨酸能和 5-羟色胺能系统的能力。据报道，MXE 还具有镇痛作用。这些发现展示了 MXE 的一些“可取品质”，并表明其可能具有治疗用途。在本文中，我们回顾了提供有关 MXE 的不良和潜在治疗作用的见解的研究结果。我们编译了关于 MXE 的毒性、致幻作用和滥用潜力，以及其有前途的抗抑郁和镇痛特性的研究。我们还讨论了可能介导观察到的有些矛盾作用的作用机制。重要的是，这篇综述为未来的研究提供了有关 MXE 的有价值信息，并将有助于更好地理解其精神药理学特性和导致其独特作用的机制。
