封锁的影响由大麻素受体拮抗剂SR141716 CB1-selective吸食大麻。
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Huestis马,Gorelick哒,Heishman SJ,普雷斯顿KL,纳尔逊RA, Moolchan ET,弗兰克RA
封锁的影响由大麻素受体拮抗剂SR141716 CB1-selective吸食大麻。
拱创精神病学。2001年4月,58 (4):322 - 8。
- PubMed ID
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11296091 (在PubMed]
- 文摘
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背景:SR141716,最近开发了CB1大麻素受体拮抗剂,街区的急性影响Delta-9-tetrahydrocannabinol (THC)和其他CB1大麻素受体激动剂在体外和动物。这些发现表明,CB1受体调节许多大麻的影响,但这尚未评估在人类。方法:六十三名健康男性吸食大麻的历史被随机分配接受口服SR141716或者安慰剂在不断升级的剂量(1、3、10、30和90毫克)的设计。每个主题抽一个活跃的THC(2.64%)或安慰剂大麻烟2小时后。与大麻中毒相关的心理影响和心率测量之前和之后的拮抗剂和大麻。结果:单剂量口服SR141716产生了明显的剂量依赖性的封锁marijuana-induced主观中毒和心动过速。90毫克剂量产生视觉模拟量表评分减少38%至43%的“你觉得现在多高?”"How stoned on marijuana are you now?" and "How strong is the drug effect you feel now?" and produced a 59% reduction in heart rate. SR141716 alone produced no significant physiological or psychological effects and did not affect peak THC plasma concentration or the area under the time x concentration curve. SR141716 was well tolerated by all subjects. CONCLUSIONS: SR141716 blocked acute psychological and physiological effects of smoked marijuana without altering THC pharmacokinetics. These findings confirm, for the first time in humans, the central role of CB1 receptors in mediating the effects of marijuana.
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