COMPARATIVE PHARMACOLOGY OF DELTA-9-TETRAHYDROCANNABINOL AND ITS METABOLITE, 11-OH-DELTA-9-TETRAHYDROCANNABINOL
COMPARATIVE PHARMACOLOGY OF DELTA-9-TETRAHYDROCANNABINOL AND ITS METABOLITE, 11-OH-DELTA-9-TETRAHYDROCANNABINOL
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DOI：
10.1172/jci107431
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发表时间：
1973-01-01
影响因子：
15.9
通讯作者：
ROWE, H
中科院分区：
文献类型：
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作者：
LEMBERGER, L;MARTZ, R;ROWE, H
对 9 名休闲大麻吸烟者进行了静脉注射 Δ9-四氢大麻酚 (Δ9-THC) 和 11-羟基-Δ9-四氢大麻酚 (11-OH-Δ9-THC) 的心理和生理影响的比较。静脉注射后 3-5 分钟内出现明显的心动过速和心理“高亢”。向所有受试者施用 11-OH-Δ9-THC (1 mg)。相比之下，心理“兴奋”的峰值在静脉注射后延迟了 10-20 分钟。施用 Δ9-THC（1 毫克）。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 [3H]11-OH-Δ9-THC 血浆水平密切相关。 [3H]11-OH-Δ9-THC 给药后，约 75% 的放射性剂量通过尿液 (25%) 和粪便 (50%) 排出。 [3H]11-OH-Δ9-THC 的处置、排泄和代谢似乎与之前报道的[14C]Δ9-THC 给药后的情况相似。这些发现，再加上 11-OH-Δ9-THC 后出现的显着心理高潮，表明在人类中，大麻中的活性成分 Δ9-THC 转化为 11-OH-Δ9-THC，这在一定程度上造成了心理影响。
A comparison of the psychologic and physiologic effects of intravenously administered Δ9-tetrahydrocannabinol (Δ9-THC) and 11-hydroxy-Δ9-tetrahydrocannabinol (11-OH-Δ9-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-Δ9-THC (1 mg) to all subjects. In contrast, the peak psychologic “high” was delayed 10-20 min after the i.v. administration of Δ9-THC (1 mg). There was some individual variation in response among subjects. Psychologic effects correlated well with plasma levels of unchanged [3H]11-OH-Δ9-THC. About 75% of the administered radioactive dose was excreted in urine (25%) and feces (50%) after [3H]11-OH-Δ9-THC administration. The disposition, excretion, and metabolism of [3H]11-OH-Δ9-THC appear to be similar to that previously reported after [14C]Δ9-THC administration. These findings, in conjunction with the marked psychologic high seen after 11-OH-Δ9-THC, suggest that in man, Δ9-THC, the active constituent in marihuana, is converted to 11-OH-Δ9-THC, which is in part responsible for the psychologic effects.Images