Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., Purdue University, West Lafayette, IN 47906-2091, USA.
Neuropharmacology. 2011 Sep;61(3):503-12. doi: 10.1016/j.neuropharm.2011.02.006. Epub 2011 Feb 23.
Many people who take LSD experience a second temporal phase of LSD intoxication that is qualitatively different, and was described by Daniel Freedman as "clearly a paranoid state." We have previously shown that the discriminative stimulus effects of LSD in rats also occur in two temporal phases, with initial effects mediated by activation of 5-HT(2A) receptors (LSD30), and the later temporal phase mediated by dopamine D2-like receptors (LSD90). Surprisingly, we have now found that non-competitive NMDA antagonists produced full substitution in LSD90 rats, but only in older animals, whereas in LSD30, or in younger animals, these drugs did not mimic LSD. Chronic administration of low doses of LSD (>3 months, 0.16 mg/kg every other day) induces a behavioral state characterized by hyperactivity and hyperirritability, increased locomotor activity, anhedonia, and impairment in social interaction that persists at the same magnitude for at least three months after cessation of LSD treatment. These behaviors, which closely resemble those associated with psychosis in humans, are not induced by withdrawal from LSD; rather, they are the result of neuroadaptive changes occurring in the brain during the chronic administration of LSD. These persistent behaviors are transiently reversed by haloperidol and olanzapine, but are insensitive to MDL-100907. Gene expression analysis data show that chronic LSD treatment produced significant changes in multiple neurotransmitter system-related genes, including those for serotonin and dopamine. Thus, we propose that chronic treatment of rats with low doses of LSD can serve as a new animal model of psychosis that may mimic the development and progression of schizophrenia, as well as model the established disease better than current acute drug administration models utilizing amphetamine or NMDA antagonists such as PCP.
许多服用 LSD 的人会经历第二 temporal 期 LSD 中毒,其性质不同,丹尼尔·弗里德曼(Daniel Freedman)将其描述为“显然是偏执状态”。我们之前已经表明,LSD 在大鼠中的辨别刺激作用也发生在两个 temporal 期,初始作用是通过激活 5-HT(2A)受体(LSD30)介导的,而后期 temporal 期是通过多巴胺 D2 样受体(LSD90)介导的。令人惊讶的是,我们现在发现,非竞争性 NMDA 拮抗剂在 LSD90 大鼠中完全替代,但仅在老年动物中,而在 LSD30 或年幼动物中,这些药物不能模拟 LSD。慢性给予低剂量 LSD(>3 个月,每隔一天 0.16mg/kg)可诱导一种行为状态,其特征为多动和易激惹、运动活动增加、快感缺失和社交互动受损,这种状态在停止 LSD 治疗后至少持续三个月保持相同的幅度。这些行为与人类精神病密切相关,不会因 LSD 戒断而引起,而是由于在慢性给予 LSD 期间大脑中发生的神经适应性变化所致。这些持续性行为可被氟哌啶醇和奥氮平短暂逆转,但对 MDL-100907 不敏感。基因表达分析数据表明,慢性 LSD 处理会导致多个神经递质系统相关基因的显著变化,包括 5-羟色胺和多巴胺基因。因此,我们提出,用低剂量 LSD 慢性治疗大鼠可以作为一种新的精神病动物模型,该模型可能模拟精神分裂症的发展和进展,并且比当前利用安非他命或 NMDA 拮抗剂(如 PCP)进行急性药物给药的模型更好地模拟已建立的疾病。