Cannon J G, Raghupathi R, Moe S T, Johnson A K, Long J P
Division of Medicinal and Natural Products Chemistry, College of Pharmacy, University of Iowa, Iowa City 52242.
J Med Chem. 1993 May 14;36(10):1316-8. doi: 10.1021/jm00062a002.
The subject compounds were prepared as a part of a continuing structure-activity study of the contrasting actions (agonism-antagonism) of (+)- and (-)-11-hydroxy-10-methylaporphine at serotonin (5-HT1A) receptors. None of the targeted nonoxygenated aporphine derivatives demonstrated significant activity in assays for any effects at serotonin 5-HT1A receptors. It is concluded that, in the aporphine series, serotonergic agonist or antagonism requires an alkyl group ortho to a phenolic OH group in the A ring.
作为对（+）-和（-）-11-羟基-10-甲基阿朴啡在5-羟色胺（5-HT1A）受体上的相反作用（激动-拮抗）进行持续构效关系研究的一部分，制备了目标化合物。在针对5-羟色胺5-HT1A受体的任何效应的测定中，没有一种目标非氧化阿朴啡衍生物表现出显著活性。得出的结论是，在阿朴啡系列中，5-羟色胺能激动或拮抗作用需要A环中酚羟基邻位有一个烷基。
