Glennon R A, Schubert E, Jacyno J M, Rosecrans J A
J Med Chem. 1980 Nov;23(11):1222-6. doi: 10.1021/jm00185a014.
Several 7-substituted derivatives of N,N-dimethyltryptamine (DMT) were prepared and evaluated in the rat fundus serotonin receptor assay and in a behavioral (discriminative stimulus) assay in rats. Both 7-Me- and 5-OMe-7-Me-DMT possess a higher pA2, and 5,7-(OMe)2-DMT a lower pA2, than that of DMT itself. Like DMT, all three of these compounds produce behavioral effects in rats which are similar to those of the hallucinogen 5-OMe-DMT. Although 7-ET- and 7-Br-DMT possess a higher serotonin receptor affinity than DMT, neither produce behavioral effects which parallel those of 5-OMe-DMT. In contrast, 6-Me-DMT and its 5-OMe derivative do not interact with the serotonin receptors in a competitive manner and are inactive in the discriminative stimulus assay.
制备了几种N，N-二甲基色胺（DMT）的7-取代衍生物，并在大鼠眼底血清素受体测定和大鼠行为（辨别刺激）测定中进行了评估。与DMT本身相比，7-甲基-DMT和5-甲氧基-7-甲基-DMT均具有更高的pA2，而5,7-（二甲氧基）-DMT的pA2更低。与DMT一样，这三种化合物在大鼠中均产生行为效应，类似于致幻剂5-甲氧基-DMT的行为效应。尽管7-乙基-DMT和7-溴-DMT比DMT具有更高的血清素受体亲和力，但两者均未产生与5-甲氧基-DMT平行的行为效应。相比之下，6-甲基-DMT及其5-甲氧基衍生物不会以竞争性方式与血清素受体相互作用，并且在辨别刺激试验中无活性。
