Addiction and Pharmacology Research Laboratory, California Pacific Medical Center Research Institute, San Francisco, CA, USA.
Psychopharmacology (Berl). 2011 Apr;214(4):933-9. doi: 10.1007/s00213-010-2103-5. Epub 2010 Dec 8.
Salvinorin A (SA) is a highly selective kappa opioid receptor agonist and the putative psychoactive compound in Salvia divinorum (SD), an increasingly abused hallucinogenic plant.
The objectives of this study were to characterize the physiological and subjective effects of SA versus placebo and measure drug and metabolite levels.
Sublingual SA doses up to 4 mg were administered in dimethyl sulfoxide/polyethylene glycol 400 solution to eight SD-experienced subjects using a placebo-controlled ascending-dose design.
No dose of SA produced significantly greater physiological or subjective effects than placebo. Furthermore, effects did not resemble reported "typical" effects of smoked SD. SA was detectable in plasma and urine, but was, in most cases, below the reliable limit of quantification (0.5 ng/mL).
Our results suggest that the sublingual bioavailability of SA is low. Higher doses, alternate formulations, or alternate routes of administration will be necessary to study the effects of SA in humans.
紫堇拉因 A（SA）是一种高选择性 κ 阿片受体激动剂，也是迷幻植物圣麻（SD）中潜在的精神活性化合物。
本研究旨在描述 SA 相对于安慰剂的生理和主观效应，并测量药物和代谢物水平。
使用安慰剂对照递增剂量设计，将高达 4 毫克的 SA 舌下剂量以二甲基亚砜/聚乙二醇 400 溶液的形式给予 8 名有 SD 经验的受试者。
没有剂量的 SA 比安慰剂产生更显著的生理或主观效应。此外，这些效应与报告的“典型”吸烟 SD 效应并不相似。SA 可在血浆和尿液中检测到，但在大多数情况下，低于可靠的定量下限（0.5ng/mL）。
我们的结果表明，SA 的舌下生物利用度较低。需要更高的剂量、不同的制剂或给药途径来研究 SA 在人类中的作用。
