The development of 5-HT_2A receptor agonists has been considerably marginalized since the demonstration that the tryptaminergic drugs, LSD and psilocybin, or the phenylakylamine drugs, mescaline and DOI, exert their hallucinogenic properties via the stimulation of 5-HT_2A receptors. Nonetheless, the ability of drugs to stimulate 5-HT_2A receptors is not necessarily associated with psychedelic experience and the hallucinogenic properties are still not understood. Several studies have increased interest in stimulating 5-HT_2A receptors in various CNS diseases. (7R)-3-bromo-2, 5-dimethoxy-bicyclo[4.2.0]octa-1,3,5-trien-7-yl]methanamine (TCB-2) which was synthetized in 2006 presents a high affinity with human and rat 5-HT_2A receptors. Its main feature of interest is that it preferentially stimulates the phospholipase C and not phospholipase A2 pathway, which is at variance with several hallucinogenic drugs. Preference for TCB-2 has increased in preclinical studies and it exhibits subtle differences compared to DOI or LSD in some molecular, cellular and behavioral studies. The purpose of this review is to take a position on the use of TCB-2 as a pharmacological tool. A careful reading of the literature has revealed that the suspected hallucinogenic properties of TCB-2 cannot firmly be ascertained while its pharmacological profile is unknown and likely not selective at 5-HT_2A receptors.

This article is part of the Special Issue entitled ‘Psychedelics: New Doors, Altered Perceptions’.

自从证明色胺能药物LSD和psilocybin或苯甲酰胺药物mescaline和DOI通过刺激5-HT _2A受体发挥致幻特性以来，5-HT _2A受体激动剂的开发已被大大边缘化。尽管如此，药物刺激5-HT _2A受体的能力并不一定与迷幻经历有关，并且仍不清楚致幻特性。几项研究对刺激各种中枢神经系统疾病中的5-HT _2A受体引起了越来越多的兴趣。2006年合成的（7R）-3-bromo-2，5-二甲氧基-双环[4.2.0] octa-1,3,5-trien-7-基]甲胺（TCB-2）与人类和大鼠5-HT _2A受体。它感兴趣的主要特征是它优先刺激磷脂酶C而不刺激磷脂酶A2途径，这与几种致幻药不同。在临床前研究中，对TCB-2的偏爱有所增加，并且在某些分子，细胞和行为研究中，与DOI或LSD相比，它表现出细微的差异。这篇综述的目的是就使用TCB-2作为药理学工具采取立场。仔细阅读文献后发现，虽然其药理作用尚不清楚，并且可能对5-HT _2A受体没有选择性，但无法可靠地确定TCB-2的致幻性。

本文是名为“迷幻分子：新门，改变观念”的特刊的一部分。