Salvinorin A is the main bioactive compound in Salvia divinorum, an endemic plant with ancestral use by the inhabitants of the Mazateca mountain range (Sierra Mazateca) in Oaxaca, México. The main use of la pastora, as locally known, is in spiritual rites due to its extraordinary hallucinogenic effects. Being the first known nonalkaloidal opioid-mediated psychotropic molecule, salvinorin A set new research areas in neuroscience. The absence of a protonated amine group, common to all previously known opioids, results in a fast metabolism with the concomitant fast elimination and swift loss of activity. The worldwide spread and psychotropic effects of salvinorin A account for its misuse and classification as a drug of abuse. Consequently, salvinorin A and Salvia divinorum are now banned in many countries. Several synthetic efforts have been focused on the improvement of physicochemical and biological properties of salvinorin A: from total synthesis to hundreds of analogues. In this Review, we discuss the impact of salvinorin A in chemistry and neuroscience covering the historical relevance, isolation from natural sources, synthetic efforts, and pharmacological and safety profiles. Altogether, the chemistry behind and the taboo that encloses salvinorin A makes it one of the most exquisite naturally occurring drugs.

中文翻译：

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化学神经科学中的黑暗经典：Salvinorin A

Salvinorin A 是迷幻鼠尾草中的主要生物活性化合物，迷幻鼠尾草是墨西哥瓦哈卡州马萨特卡山脉 (Sierra Mazateca) 居民祖传使用的地方性植物。众所周知，la pastora主要用于精神仪式，因为它具有非凡的致幻作用。作为第一个已知的非生物碱类阿片类药物介导的精神药物分子，salvinorin A 在神经科学领域开辟了新的研究领域。质子化胺基团的缺失是所有先前已知的阿片样物质所共有的，导致快速新陈代谢，伴随着快速消除和迅速丧失活性。salvinorin A 在世界范围内的传播和精神作用导致其被滥用并被归类为滥用药物。因此，salvinorin A 和Salvia divinorum现在很多国家都禁止了。一些合成工作集中在改善 salvinorin A 的物理化学和生物学特性：从全合成到数百种类似物。在这篇综述中，我们讨论了 salvinorin A 在化学和神经科学中的影响，包括历史相关性、与天然来源的分离、合成努力以及药理学和安全性概况。总而言之，salvinorin A 背后的化学原理和禁忌使其成为最精致的天然药物之一。