Glennon R A, Gessner P K
J Med Chem. 1979 Apr;22(4):428-32. doi: 10.1021/jm00190a014.
Using a rat fundus model, the serotonin (5-HT) receptor binding affinities of 27 tryptamine analogues were determined. Factors which might affect affinity were examined, e.g., lipids solubility, as reflected by partition coefficient, and pKa. Structure-activity relationships were developed and are discussed in terms of substituents on the terminal amine, the side chain, and the indole 1 position, the 5 position, and at other positions on the indolic nucleus. If lipid solubility and metabolism can be accounted for, there appears to be a parallelism between 5-HT receptor binding affinities and the hallucinogenic (psychotomimetic) potencies of several of these compounds.
利用大鼠眼底模型，测定了27种色胺类似物的血清素（5-羟色胺，5-HT）受体结合亲和力。研究了可能影响亲和力的因素，例如由分配系数反映的脂溶性和pKa。建立了构效关系，并根据末端胺、侧链以及吲哚1位、5位和吲哚核上其他位置的取代基进行了讨论。如果能够解释脂溶性和代谢情况，那么其中几种化合物的5-HT受体结合亲和力与致幻（拟精神病）效力之间似乎存在平行关系。
