Exogenous Delta9-Tetrahydrocannabinol Influences Circulating Endogenous Cannabinoids in Humans
Exogenous Delta9-Tetrahydrocannabinol Influences Circulating Endogenous Cannabinoids in Humans
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外源性 Delta9-四氢大麻酚影响人体循环内源性大麻素
DOI：
10.1097/jcp.0b013e3182984015
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发表时间：
2013
影响因子：
2.9
通讯作者：
Lötsch J.
中科院分区：
文献类型：
--
作者：
Walter C;Ferreirós N;Bishay P;Geisslinger G;Tegeder I;Lötsch J.
Delta 9-四氢大麻酚(THC)与内源性大麻素花生四烯酸乙醇胺(Anandamide)和2-花生四氢大麻酰甘油(2-AG)在大麻素受体上竞争。这可能会导致内源性大麻素信号级联的适应性变化，从而可能对内源性大麻素系统的生物学功能产生影响。我们发现，与安慰剂相比，30名健康志愿者单次口服20 mg THC后2小时和3小时的循环中ANANDAME、2-AG、棕榈酰乙醇胺和油酰乙醇胺的浓度较高。在给药后2小时，油酰乙醇胺的血药浓度变化与血药浓度呈线性相关。在大鼠中，CB1/CB2激动剂Win 55,212的治疗也增加了血浆内源性大麻素的浓度。然而，这与特定脑区(包括脊髓、皮质和下丘脑)中乙醇胺内源性大麻素的减少有关；而皮质中2-花生四烯酸甘油的含量增加。因此，给志愿者服用THC影响了循环中的内源性大麻素的浓度，这与Win-55,212在大鼠中的模拟结果相似，表明外源性大麻素可能会导致可在血浆中检测到的内源性大麻素系统的变化。
Delta 9-tetrahydrocannabinol (THC) competes with the endogenous cannabinoids arachidonoyl ethanolamide (anandamide) and 2-arachidonoyl glycerol (2-AG) at cannabinoid receptors. This may cause adaptive changes in the endocannabinoid signaling cascade with possible consequences for the biological functions of the endocannabinoid system. We show that administration of a single oral dose of 20 mg THC to 30 healthy volunteers resulted in higher circulating concentrations of anandamide, 2-AG, palmitoyl ethanolamide, and oleoylethanolamide at 2 and 3 hours after administration as compared with placebo. At 2 hours after THC administration, changes in oleoylethanolamide plasma concentrations from baseline were linearly related to the THC plasma concentrations. In rats, treatment with the CB 1/CB 2 agonist WIN 55,212 also increased plasma endocannabinoid concentrations. However, this was associated with a decrease of ethanolamide endocannabinoids in specific brain regions including spinal cord, cortex, and hypothalamus; whereas 2-arachidonoyl glycerol increased in the cortex. Thus, administration of THC to human volunteers influenced the concentrations of circulating endocannabinoids, which was mimicked by WIN-55,212 in rats, suggesting that exogenous cannabinoids may lead to changes in the endocannabinoid system that can be detected in plasma.
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DOI：
10.1006/bbrc.2000.2406
发表时间：
2000-04-02
影响因子：
3.1
作者：
González, S;Bisogno, T;Fernández-Ruiz, JJ
通讯作者：
Fernández-Ruiz, JJ
CYP2C 参与老妇人肝微粒体的大麻素代谢。
影响因子：
2
作者：
Kazuhito Watanabe;T. Matsunaga;I. Yamamoto;Y. Funae;H. Yoshimura
通讯作者：
H. Yoshimura
影响因子：
7.3
作者：
Maccarrone, M.
通讯作者：
Maccarrone, M.
影响因子：
6.1
作者：
Yamaori, Satoshi;Ebisawa, Juri;Watanabe, Kazuhito
通讯作者：
Watanabe, Kazuhito
Δ9-四氢大麻酚的血浆浓度是否反映了中毒程度？
DOI：
--
发表时间：
1981
期刊：
影响因子：
--
作者：
Leo E. Hollister;H. Gillespie;A. Ohlsson;Jan;A. Wahlén;S. Agurell;S. Agurell
通讯作者：
S. Agurell