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化学神经科学经典:蝇蕈醇。

Classics in Chemical Neuroscience: Muscimol.

机构信息

Bioactive Heterocycles Synthesis Laboratory (BHSL), Departamento de Farmacia, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Avenida Vicuña Mackenna 4860, Macul, Santiago 7820436, Chile.

Centro Interdisciplinario de Neurociencias, Pontificia Universidad Católica de Chile, Marcoleta 391, Santiago 8330024, Chile.

出版信息

ACS Chem Neurosci. 2024 Sep 18;15(18):3257-3269. doi: 10.1021/acschemneuro.4c00304. Epub 2024 Sep 10.

Abstract

Muscimol () is a psychoactive isoxazole present in various mushrooms, along with ibotenic acid and muscarine. It is structurally related to GABA and acts as a GABA agonist with great affinity. Muscimol use dates back to Siberian shamanic cultures as an entheogen, where it was ingested orally to exert psychoactive effects. Although not approved for clinical use, its potential and use as a research tool in neuroscience is of immense value, with H-muscimol being used as a radioligand in GABA receptor research. Since its discovery in the early 60s, many research groups have worked on the synthesis of the compound. Recent research suggests the potential use of muscimol in neuropathic pain relief and other potential uses are also being studied. In this review, we will cover the history, chemistry, pharmacology and overall importance of the compound.

摘要

蝇蕈醇()是一种存在于各种蘑菇中的具有精神活性的异噁唑,与 蕈氨酸和毒蕈碱一起存在。它在结构上与 GABA 相关,作为 GABA 激动剂具有很大的亲和力。蝇蕈醇的使用可以追溯到西伯利亚萨满教文化作为一种致幻剂,在那里它被口服摄入以发挥精神活性作用。尽管尚未批准用于临床用途,但它作为神经科学研究工具的潜力和用途具有巨大的价值,H-蝇蕈醇被用作 GABA 受体研究中的放射性配体。自 20 世纪 60 年代初发现以来,许多研究小组一直在致力于该化合物的合成。最近的研究表明蝇蕈醇在治疗神经性疼痛方面具有潜在的用途,其他潜在用途也在研究中。在这篇综述中,我们将介绍该化合物的历史、化学、药理学和总体重要性。

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