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3H-δ9-四氢大麻酚、3H-大麻酚和3H-大麻二酚:在大鼠脑中的渗透及区域分布

3H-delta 9-Tetrahydrocannabinol, 3H-cannabinol and 3H-cannabidiol: penetration and regional distribution in rat brain.

作者信息

Alozie S O, Martin B R, Harris L S, Dewey W L

出版信息

Pharmacol Biochem Behav. 1980 Feb;12(2):217-21. doi: 10.1016/0091-3057(80)90359-7.

DOI:10.1016/0091-3057(80)90359-7
PMID:6246544
Abstract

3H-delta 9-Tetrahydrocannabinol (3H-delta 9-THC), 3H-cannabidiol (3H-CBD) and 3H-cannabinol (3H-CBN) were administered (1 mg/kg) to male rats which were decapitated either 0.5, 1, 15, 30 or 90 min later. The plasma concentration was similar for all cannabinoids throughout the time course. After 5 min greater than 80% of the plasma radioactivity in each treatment was due to metabolites. Radioactivity rapidly entered brain after the administration of 3H-CBD, 3H-CBN, and 3H-delta 9-THC. The concentrations of unchanged 3H-CBD aand 3H-CBN in whole brain were higher than that of 3H-delta 9-THC 5 min after administration. Regional distribution of radioactivity in the brain after 5 min was similar for all three cannabinoids, the only significant difference being in hypothalamus. Coadministration of 3H-delta 9-THC with a five-fold excess of either CBD or delta 9-THC did not produce any significant alteration in the levels of radioactivity in brain or plasma 5 min after their injection. The difference in behavioral activity of delta 9-THC, CBD and CBN cannot be explained by penetrability or regional distribution in the brain.

摘要

将3H-δ9-四氢大麻酚(3H-δ9-THC)、3H-大麻二酚(3H-CBD)和3H-大麻酚(3H-CBN)(1毫克/千克)给予雄性大鼠,在给药后0.5、1、15、30或90分钟将其断头。在整个时间过程中,所有大麻素的血浆浓度相似。5分钟后,各处理中超过80%的血浆放射性归因于代谢物。给予3H-CBD、3H-CBN和3H-δ9-THC后,放射性迅速进入大脑。给药5分钟后,全脑中未变化的3H-CBD和3H-CBN的浓度高于3H-δ9-THC。5分钟后,三种大麻素在脑中的放射性区域分布相似,唯一显著差异在于下丘脑。将3H-δ9-THC与五倍过量的CBD或δ9-THC共同给药后,注射5分钟后脑中或血浆中的放射性水平未产生任何显著变化。δ9-THC、CBD和CBN在行为活性上的差异无法通过其在脑中的穿透性或区域分布来解释。

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