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在人类中,κ 阿片样物质激动剂 Salvinorin A 的剂量相关的行为、主观、内分泌和心理生理效应。

Dose-related behavioral, subjective, endocrine, and psychophysiological effects of the κ opioid agonist Salvinorin A in humans.

机构信息

Psychiatry Service, Veterans Affairs Connecticut Healthcare System, West Haven, CT 06516, USA.

出版信息

Biol Psychiatry. 2012 Nov 15;72(10):871-9. doi: 10.1016/j.biopsych.2012.06.012. Epub 2012 Jul 18.

DOI:10.1016/j.biopsych.2012.06.012
PMID:22817868
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3638802/
Abstract

BACKGROUND

Salvia divinorum (Salvia) is an increasingly popular recreational drug amongst adolescents and young adults. Its primary active ingredient, Salvinorin A (SA)-a highly selective agonist at the κ opiate receptor-is believed to be one of the most potent naturally occurring hallucinogens. However, there is little experimental data on the effects of SA in humans.

METHODS

In a 3-day, double-blind, randomized, crossover, counterbalanced study, the behavioral, subjective, cognitive, psychophysiological, and endocrine effects of 0 mg, 8 mg, and 12 mg of inhaled SA were characterized in 10 healthy individuals who had previously used Salvia.

RESULTS

SA produced psychotomimetic effects and perceptual alterations, including dissociative and somaesthetic effects, increased plasma cortisol and prolactin, and reduced resting electroencephalogram spectral power. The SA administration was associated with a rapid increase of its levels in the blood. SA did not produce euphoria, cognitive deficits, or changes in vital signs. The effects were transient and not dose-related. SA administration was very well-tolerated without acute or delayed adverse effects.

CONCLUSIONS

SA produced a wide range of transient effects in healthy subjects. The perceptual altering effects and lack of euphoric effects would explain its intermittent use pattern. Such a profile would also suggest a low addictive potential similar to other hallucinogens and consistent with κ opiate receptor agonism. Further work is warranted to carefully characterize a full spectrum of its effects in humans, to elucidate the underlying mechanisms involved, and to explore the basis for individual variability in its effects.

摘要

背景

迷幻鼠尾草(Salvia divinorum)是青少年和年轻人中越来越流行的消遣性药物。其主要活性成分,即 Salvinorin A(SA),是κ阿片受体的高选择性激动剂,被认为是最有效的天然致幻剂之一。然而,关于 SA 在人体中的作用的实验数据很少。

方法

在一项为期 3 天的、双盲、随机、交叉、平衡对照研究中,10 名曾使用过迷幻鼠尾草的健康个体接受了 0mg、8mg 和 12mg 吸入式 SA 的处理,评估其行为、主观、认知、心理生理和内分泌效应。

结果

SA 产生了精神病样效应和知觉改变,包括分离和躯体感觉效应,增加了血浆皮质醇和催乳素水平,并降低了静息脑电图的频谱功率。SA 的给药与血液中其水平的快速增加有关。SA 没有产生欣快感、认知缺陷或生命体征变化。效应是短暂的,与剂量无关。SA 的给药耐受性良好,没有急性或迟发性不良反应。

结论

SA 在健康个体中产生了广泛的短暂效应。知觉改变效应和缺乏欣快感效应可以解释其间歇性使用模式。这种特征还表明,它与其他致幻剂一样,具有较低的成瘾潜力,与 κ 阿片受体激动剂作用一致。进一步的工作需要仔细描述其在人体中的全谱效应,阐明涉及的潜在机制,并探索其效应个体差异的基础。

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