Univ Rennes, INSERM, INRAE, CHU Rennes, Institut NuMeCan (Nutrition, Métabolisme et Cancer), F-35000 Rennes, France.
Centre Hospitalier Universitaire de Rennes, Laboratoire de Toxicologie Biologique et Medico-Légale, CHU Pontchaillou, 2 Rue Henri Le Guilloux, F-35000 Rennes, France.
Int J Mol Sci. 2022 Dec 8;23(24):15574. doi: 10.3390/ijms232415574.
Since the 2000s, an increasing number of new psychoactive substances (NPS) have appeared on the drug market. Arylcyclohexylamine (ACH) compounds such as ketamine, phencyclidine and eticyclidine derivatives are of particular concern, given their rapidly increasing use and the absence of detailed toxicity data. First used mainly for their pharmacological properties in anesthesia, their recreational use is increasing. ACH derivatives have an antagonistic activity against the N-methyl-D-aspartate receptor, which leads to dissociative effects (dissociation of body and mind). Synthetic ketamine derivatives produced in Asia are now arriving in Europe, where most are not listed as narcotics and are, thus, legal. These structural derivatives have pharmacokinetic and pharmacodynamic properties that are sometimes very different from ketamine. Here, we describe the pharmacology, epidemiology, chemistry and metabolism of ACH derivatives, and we review the case reports on intoxication.
自 21 世纪以来,越来越多的新型精神活性物质(NPS)出现在毒品市场上。芳基环己基胺(ACH)化合物,如氯胺酮、苯环利定和乙环利定衍生物,因其使用量迅速增加且缺乏详细的毒性数据而备受关注。ACH 衍生物最初主要因其在麻醉中的药理学特性而被使用,但其娱乐用途正在增加。ACH 衍生物对 N-甲基-D-天冬氨酸受体具有拮抗活性,导致分离效应(身心分离)。亚洲生产的合成氯胺酮衍生物现已进入欧洲,在欧洲,这些物质大多未被列为麻醉品,因此是合法的。这些结构衍生物具有有时与氯胺酮非常不同的药代动力学和药效学特性。在这里,我们描述了 ACH 衍生物的药理学、流行病学、化学和代谢,并回顾了关于中毒的病例报告。