NBOMes——LSD 的强效有毒替代品,Frontiers in Neuroscience

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NBOMes——LSD 的强效有毒替代品
Frontiers in Neuroscience ( IF 3.2 ) Pub Date : 2020-02-26 , DOI: 10.3389/fnins.2020.00078
Jolanta B Zawilska ₁ , Monika Kacela ₁ , Piotr Adamowicz ₂

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最近，非法毒品市场上出现了一类名为 NBOMe（或 25X-NBOMe）的新型迷幻化合物。NBOmes 是苯乙胺药物 2C 家族的类似物，最初由 Alexander Shulgin 合成，含有 N-（2-甲氧基）苄基取代基。该组中最常报告的药物是 25I-NBOMe、25B-NBOMe 和 25C-NBOMe。NBOMe 化合物是血清素 5-HT2A 和 5-HT2C 受体（低纳摩尔范围的 Ki 值）的超强效和高效激动剂，与 5-HT1A 相比，对 5-HT2A 的选择性超过 1000 倍。与 5-HT2A 或 5-HT2C 相比，它们对 5-HT2A 受体的亲和力高于其 2C 对应物，并且对 5-HT2B 受体的亲和力、效力和功效明显较低。这些药物以吸墨纸或粉末、液体或片剂形式出售，它们通过舌下/口腔、静脉内、鼻腔吹气或吸烟给药。自 2010 年代初推出以来，已发表了大量关于因食用 NBOMe 化合物而导致的临床中毒和死亡的报告。常见的不良反应包括幻视和幻听、混乱、焦虑、恐慌和恐惧、激动、无法控制的暴力行为、癫痫发作、兴奋性谵妄和拟交感神经症状，如瞳孔扩大、心动过速、高血压、体温过高和出汗。还报告了横纹肌溶解、弥散性血管内凝血、低血糖、代谢性酸中毒和多器官衰竭。该调查提供了与 NBOMe 使用相关的药理特性、使用模式、代谢和预期效果的最新概述。特别强调涉及这些化合物的非致命和致命中毒案例。即使对于应用现代敏感技术的实验室来说，生物材料中 NBOM 的分析也具有挑战性，因此本文还介绍了最常用于检测和鉴定 NBOM 及其代谢物的分析方法。

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NBOMes–Highly Potent and Toxic Alternatives of LSD

Recently, a new class of psychedelic compounds named NBOMe (or 25X-NBOMe) has appeared on the illegal drug market. NBOMes are analogs of the 2C family of phenethylamine drugs, originally synthesized by Alexander Shulgin, that contain a N-(2-methoxy)benzyl substituent. The most frequently reported drugs from this group are 25I-NBOMe, 25B-NBOMe, and 25C-NBOMe. NBOMe compounds are ultrapotent and highly efficacious agonists of serotonin 5-HT2A and 5-HT2C receptors (Ki values in low nanomolar range) with more than 1000-fold selectivity for 5-HT2A compared with 5-HT1A. They display higher affinity for 5-HT2A receptors than their 2C counterparts and have markedly lower affinity, potency, and efficacy at the 5-HT2B receptor compared to 5-HT2A or 5-HT2C. The drugs are sold as blotter papers, or in powder, liquid, or tablet form, and they are administered sublingually/buccally, intravenously, via nasal insufflations, or by smoking. Since their introduction in the early 2010s, numerous reports have been published on clinical intoxications and fatalities resulting from the consumption of NBOMe compounds. Commonly observed adverse effects include visual and auditory hallucinations, confusion, anxiety, panic and fear, agitation, uncontrollable violent behavior, seizures, excited delirium, and sympathomimetic signs such mydriasis, tachycardia, hypertension, hyperthermia, and diaphoresis. Rhabdomyolysis, disseminated intravascular coagulation, hypoglycemia, metabolic acidosis, and multiorgan failure were also reported. This survey provides an updated overview of the pharmacological properties, pattern of use, metabolism, and desired effects associated with NBOMe use. Special emphasis is given to cases of non-fatal and lethal intoxication involving these compounds. As the analysis of NBOMes in biological materials can be challenging even for laboratories applying modern sensitive techniques, this paper also presents the analytical methods most commonly used for detection and identification of NBOMes and their metabolites.

更新日期：2020-02-26

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