Glennon R A, Young R
Pharmacol Biochem Behav. 1982 Oct;17(4):603-7. doi: 10.1016/0091-3057(82)90330-6.
Prominent among the class of hallucinogenic phenylisopropylamines is the 2,5-dimethoxy substitution pattern; this pattern has long been recognized as being an important feature of the more potent agents within this class. The purpose of this present study was to explore the behavioral properties of a series of methoxylated phenylisopropylamines in order to determine the effect of other substitution patterns and the relative importance of individual methoxy groups. Rats, trained to discriminate the hallucinogenic agent 2,5-dimethoxy-4-methyl-phenylisopropylamine (DOM) from saline in a two-lever drug discrimination task, were challenged with a series of di- and trimethoxyphenylisopropylamines (i.e., DMA and TMA derivatives). DOM-stimulus generalization was found to occur with 2,4-DMA but not with 2,3-DMA, 2.6-DMA, or 3,5-DMA; generalization also occurred with 2,3,4-TMA, 2,3,5-TMA, 2,4,6-TMA and 3,4,5-TMA. The 2,4-dimethoxy pattern also emerges as an important feature among the more active agents.
在致幻性苯异丙胺类中，2,5 - 二甲氧基取代模式尤为突出；长期以来，这种模式一直被认为是该类中更具效力的药物的一个重要特征。本研究的目的是探究一系列甲氧基化苯异丙胺的行为特性，以确定其他取代模式的影响以及各个甲氧基的相对重要性。在一项双杠杆药物辨别任务中，训练大鼠区分致幻剂2,5 - 二甲氧基 - 4 - 甲基 - 苯异丙胺（DOM）和生理盐水，然后用一系列二甲基和三甲基氧基苯异丙胺（即DMA和TMA衍生物）对其进行挑战。发现2,4 - DMA能产生DOM刺激泛化，而2,3 - DMA、2,6 - DMA或3,5 - DMA则不能；2,3,4 - TMA、2,3,5 - TMA、2,4,6 - TMA和3,4,5 - TMA也能产生泛化。2,4 - 二甲氧基模式在更具活性的药物中也呈现为一个重要特征。
