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首页> 外文期刊>The Journal of toxicological sciences >Inhibitory effect of synthetic cannabinoids on CYPIA activity in mouse liver microsomes
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Inhibitory effect of synthetic cannabinoids on CYPIA activity in mouse liver microsomes

机译：合成大麻素对小鼠肝微粒体CYPIA活性的抑制作用

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摘要

Synthetic cannabinoids developed by chemical modification are believed to bind to cannabinoid receptors and cause neurological effects similar to cannabis; however, their effects on drug metabolizing enzymes are unknown. This study aimed to elucidate the effect of synthetic cannabinoids on cytochrome P450 1A activity. Naphthoylindole, a basic structure of the major synthetic cannabinoids, strongly inhibited CYP1A activity in a competitive manner; the apparent Ki value was 0.40 mu M. The N-Alkylated derivatives of naphthoylindole, MAM-2201 and JWH-019, also inhibited CYP1A activity in a concentration-dependent manner; however, their inhibitory effects were weaker than naphthoylindole. An adamantylamidoindole derivative, STS-135, showed inhibition of CYP1A activity in a concentration-dependent manner, but the adamantoylindole derivatives, AB-001 and AM-1248, did not. A tetramethylcyclopropanoylindole derivative, UR-144, showed a weak inhibition of CYP1A activity at high concentrations. These results suggest that synthetic cannabinoids and their basic molecules are capable of inhibiting CYP1A enzymatic activity.
机译：通过化学修饰开发的合成大麻素被认为与大麻素受体结合并引起类似于大麻的神经系统作用。然而，它们对药物代谢酶的作用尚不清楚。这项研究旨在阐明合成大麻素对细胞色素P450 1A活性的影响。萘并吲哚是主要合成大麻素的基本结构，以竞争性方式强烈抑制CYP1A的活性。表观Ki值为0.40μM。萘甲吲哚的N-烷基化衍生物，MAM-2201和JWH-019也以浓度依赖的方式抑制CYP1A的活性。但是，它们的抑制作用比萘甲吲哚弱。一个金刚酰胺基吲哚衍生物STS-135以浓度依赖的方式显示出对CYP1A活性的抑制作用，但金刚烷基吲哚衍生物AB-001和AM-1248却没有。四甲基环丙酰基吲哚衍生物UR-144在高浓度下对CYP1A活性的抑制作用较弱。这些结果表明合成的大麻素及其基本分子能够抑制CYP1A的酶活性。

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