UCIBIO-REQUIMTE, Laboratório de Toxicologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313, Porto, Portugal,
Arch Toxicol. 2015 Aug;89(8):1151-73. doi: 10.1007/s00204-015-1513-x. Epub 2015 Apr 16.
In the area of psychotropic drugs, tryptamines are known to be a broad class of classical or serotonergic hallucinogens. These drugs are capable of producing profound changes in sensory perception, mood and thought in humans and act primarily as agonists of the 5-HT2A receptor. Well-known tryptamines such as psilocybin contained in Aztec sacred mushrooms and N,N-dimethyltryptamine (DMT), present in South American psychoactive beverage ayahuasca, have been restrictedly used since ancient times in sociocultural and ritual contexts. However, with the discovery of hallucinogenic properties of lysergic acid diethylamide (LSD) in mid-1900s, tryptamines began to be used recreationally among young people. More recently, new synthetically produced tryptamine hallucinogens, such as alpha-methyltryptamine (AMT), 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) and 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT), emerged in the recreational drug market, which have been claimed as the next-generation designer drugs to replace LSD ('legal' alternatives to LSD). Tryptamine derivatives are widely accessible over the Internet through companies selling them as 'research chemicals', but can also be sold in 'headshops' and street dealers. Reports of intoxication and deaths related to the use of new tryptamines have been described over the last years, raising international concern over tryptamines. However, the lack of literature pertaining to pharmacological and toxicological properties of new tryptamine hallucinogens hampers the assessment of their actual potential harm to general public health. This review provides a comprehensive update on tryptamine hallucinogens, concerning their historical background, prevalence, patterns of use and legal status, chemistry, toxicokinetics, toxicodynamics and their physiological and toxicological effects on animals and humans.
在精神药物领域，色胺类被认为是一类广泛的经典或血清素能致幻剂。这些药物能够在人类中产生感官知觉、情绪和思维的深刻变化，主要作为 5-HT2A 受体的激动剂。从古至今，在社会文化和仪式背景下，在阿兹特克圣蘑菇中发现的致幻剂蘑菇碱(psilocybin)和在南美致幻饮料 ayahuasca 中发现的 N,N-二甲基色胺(DMT)等知名色胺类药物的使用一直受到限制。然而，自 20 世纪中期发现麦角酸二乙酰胺 (LSD) 的致幻特性以来，色胺类药物开始在年轻人中被娱乐性使用。最近，一些新的合成色胺类致幻剂，如α-甲基色胺(AMT)、5-甲氧基-N,N-二甲基色胺(5-MeO-DMT)和 5-甲氧基-N,N-二异丙基色胺(5-MeO-DIPT)，出现在娱乐性药物市场上，被称为替代 LSD 的新一代设计药物(“合法”替代 LSD)。通过销售“研究用化学品”的公司，在互联网上可以广泛获取色胺类衍生物，但也可以在“头店”和街头毒贩那里买到。近年来，有关使用新型色胺类药物导致中毒和死亡的报告不断出现，引起了国际社会对色胺类药物的关注。然而，由于缺乏关于新型色胺类致幻剂的药理学和毒理学特性的文献，因此难以评估它们对公众健康的实际潜在危害。本综述全面介绍了色胺类致幻剂，包括其历史背景、流行程度、使用模式和法律地位、化学、毒代动力学、毒效动力学以及对动物和人类的生理和毒理效应。
