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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Thujone exhibits low affinity for cannabinoid receptors but fails to evoke cannabimimetic responses.
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Thujone exhibits low affinity for cannabinoid receptors but fails to evoke cannabimimetic responses.

机译：丁香酮对大麻素受体的亲和力低，但无法引起大麻素反应。

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摘要

Absinthe, an abused drug in the early 1900s, has been speculated to activate the receptors responsible for marijuana intoxication (the CB1 cannabinoid receptor) (Nature 253:365-356; 1975). To test this hypothesis, we investigated oil of wormwood (Artemisia absinthium) the active plant product found in absinthe, and thujone, the active compound found in oil of wormwood. Radioligand receptor binding assays employing membrane preparations from rat brains containing CB1 cannabinoid receptors, and human tonsils containing CB2 receptors, demonstrated that thujone displaced [3H]CP55940, a cannabinoid agonist, only at concentrations above 10 microM. HPLC analysis of oil of wormwood revealed that only the fractions having mobility close to thujone displaced [3H]CP55940 from the CB1 cannabinoid receptor. [35S]GTPgammaS binding assays revealed that thujone failed to stimulate G-proteins even at 0.1 mM. Thujone failed to inhibit forskolin-stimulated adenylate cyclase activity in N18TG2 membranes at 1 mM. Rats administered thujone exhibited different behavioral characteristics compared with rats administered a potent cannabinoid agonist, levonantradol. Therefore, the hypothesis that activation of cannabinoid receptors is responsible for the intoxicating effects of thujone is not supported by the present data.
机译：据推测，苦艾酒是1900年代初期的一种滥用药物，它可以激活引起大麻中毒的受体（CB1大麻素受体）（自然253：365-356; 1975）。为了验证这一假设，我们调查了在苦艾中发现的活性植物产品艾草（艾蒿）的油和在艾草中发现的活性化合物丁香的油。放射性配体受体结合试验采用了含有CB1大麻素受体的大鼠大脑和含有CB2受体的人扁桃体的膜制剂，结果表明，丁香酮取代了[3H] CP55940（一种大麻素激动剂），浓度只有10 microM以上。苦艾油的HPLC分析表明，只有具有接近丁香酮迁移率的馏分从CB1大麻素受体置换了[3H] CP55940。 [35S] GTPgammaS结合试验表明，即使在0.1 mM时，丁香酮也无法刺激G蛋白。 Thujone在1 mM时未能抑制N18TG2膜中福司可林刺激的腺苷酸环化酶活性。与施用强力大麻素激动剂左炔诺醇的大鼠相比，施用硫黄酮的大鼠表现出不同的行为特征。因此，当前数据不支持关于大麻素受体的激活导致丁香酮中毒作用的假设。

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