Appel J B, White F J, Holohean A M
Neurosci Biobehav Rev. 1982 Winter;6(4):529-36. doi: 10.1016/0149-7634(82)90036-7.
Some of the advantages of using drug discrimination (DD) procedure to analyze the mechanisms of action of hallucinogenic and related drugs were illustrated by reviewing research with lysergic acid diethylamide (LSD). Because they ensure that drug-induced alterations in interoceptive "state" become biologically meaningful "cues," these procedures are reliable, robust, sensitive and specific. With reference to LSD, many DD experiments suggest: (1) that while hallucinogens substitute for (mimic) LSD (in rats), such substitution does not predict hallucinogenic potency (in humans) but does predict similarities in mechanism(s) of action; (2) the behavioral (in vivo) effects of LSD, unlike those of some of its congeners, are mediated primarily by central, serotonergic (5-HT) neuronal mechanism although LSD may also have (secondary) dopamine (DA) agonist properties; (3) both the locus and the nature of these LSD-5-HT interactions are unclear: cells arising from B-7, B-8 and B-9 regions of the dorsal-medial raphe may be involved; pretreatment with agents that deplete 5-HT and increase the stereospecific binding of 3H-LSD in vitro (p-chlorophenylalanine; 5,7-dihydroxytryptamine) enhance sensitivity to LSD in vivo.
通过回顾麦角酸二乙酰胺（LSD）的研究，阐述了使用药物辨别（DD）程序分析致幻剂及相关药物作用机制的一些优势。因为这些程序能确保药物引起的内感受“状态”改变成为具有生物学意义的“线索”，所以它们可靠、稳健、灵敏且特异。关于LSD，许多DD实验表明：（1）虽然致幻剂在大鼠中可替代（模拟）LSD，但这种替代并不能预测其在人类中的致幻效力，不过能预测作用机制的相似性；（2）与某些同系物不同，LSD的行为（体内）效应主要由中枢5-羟色胺能（5-HT）神经元机制介导，尽管LSD可能也具有（次要的）多巴胺（DA）激动剂特性；（3）LSD与5-HT相互作用的位点和性质尚不清楚：可能涉及背内侧中缝核B-7、B-8和B-9区域产生的细胞；用能耗尽5-HT并在体外增加3H-LSD立体特异性结合的药物（对氯苯丙氨酸；5,7-二羟基色胺）预处理可增强体内对LSD的敏感性。
