Lemberger L, Martz R, Rodda B, Forney R, Rowe H
J Clin Invest. 1973 Oct;52(10):2411-7. doi: 10.1172/JCI107431.
A comparison of the psychologic and physiologic effects of intravenously administered Delta(9)-tetrahydrocannabinol (Delta(9)-THC) and 11-hydroxy-Delta(9)-tetrahydrocannabinol (11-OH-Delta(9)-THC) was carried out in nine casual marihuana smokers. A marked tachycardia and psychologic "high" occurred within 3-5 min after the i.v. administration of 11-OH-Delta(9)-THC (1 mg) to all subjects. In contrast, the peak psychologic "high" was delayed 10-20 min after the i.v. administration of Delta(9)-THC (1 mg). There was some individual variation in response among subjects. Psychologic effects correlated well with plasma levels of unchanged [(3)H]11-OH-Delta(9)-THC. About 75% of the administered radioactive dose was excreted in urine (25%) and feces (50%) after [(3)H]11-OH-Delta(9)-THC administration. The disposition, excretion, and metabolism of [(3)H]11-OH-Delta(9)-THC appear to be similar to that previously reported after [(14)C]Delta(9)-THC administration. These findings, in conjunction with the marked psychologic high seen after 11-OH-Delta(9)-THC, suggest that in man, Delta(9)-THC, the active constituent in marihuana, is converted to 11-OH-Delta(9)-THC, which is in part responsible for the psychologic effects.
对9名偶尔吸食大麻者进行了静脉注射Δ⁹-四氢大麻酚（Δ⁹-THC）和11-羟基-Δ⁹-四氢大麻酚（11-OH-Δ⁹-THC）的心理和生理效应比较。对所有受试者静脉注射11-OH-Δ⁹-THC（1毫克）后3-5分钟内出现明显的心动过速和心理“兴奋”。相比之下，静脉注射Δ⁹-THC（1毫克）后，心理“兴奋”峰值延迟10-20分钟。受试者之间的反应存在一些个体差异。心理效应与未变化的[(³)H]11-OH-Δ⁹-THC血浆水平密切相关。给予[(³)H]11-OH-Δ⁹-THC后，约75%的给药放射性剂量经尿液（25%）和粪便（50%）排泄。[(³)H]11-OH-Δ⁹-THC的处置、排泄和代谢似乎与先前报道的[(¹⁴)C]Δ⁹-THC给药后的情况相似。这些发现，连同11-OH-Δ⁹-THC后出现的明显心理兴奋，表明在人体内，大麻中的活性成分Δ⁹-THC转化为11-OH-Δ⁹-THC，后者部分导致了心理效应。
