Phenethylamine hallucinogens in the locus coeruleus: potency of action correlates with rank order of 5-HT2 binding affinity.
Phenethylamine hallucinogens in the locus coeruleus: potency of action correlates with rank order of 5-HT2 binding affinity.
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DOI：
10.1016/0014-2999(86)90014-2
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发表时间：
1986-12
影响因子：
5
通讯作者：
K. Rasmussen;R. Glennon;G. Aghajanian
中科院分区：
文献类型：
--
作者：
K. Rasmussen;R. Glennon;G. Aghajanian
三种苯乙胺类致幻剂对蓝斑的生理效应大小顺序与5-HT 2结合力大小顺序一致（（-）DOB > DOM >（+）DOB）。DOB的行为无活性位置异构体SL-7161对LC单元活性无显著影响。这些结果提供了深入了解5-HT 2受体的结构-活性关系，并支持早期的研究结果，即LC中显示的致幻剂的作用是通过5-HT 2受体介导的。
The rank order of potency for the physiological effects of three phenethylamine hallucinogens in the locus coeruleus (LC) was identical to that previously shown for their 5-HT2binding affinity ((-) DOB > DOM > (+)DOB). The behaviorally inactive positional isomer of DOB, SL-7161, did not significantly affect LC unit activity. These results offer insight into structure-activity relationships at 5-HT2receptors and support earlier findings that the actions of hallucinogens displayed in the LC are mediated via 5-HT2receptors.