Yang D J, Davisson J N
J Med Chem. 1985 Sep;28(9):1361-5. doi: 10.1021/jm00147a044.
Ketamine and phencyclidine are structurally similar compounds that share many pharmacological actions, some of which are similar to the phenethylamines amphetamine and cathione. In order to integrate structural features of ketamine and cathinone, two groups of analogues, which are more conformationally restricted compared to the parent compounds, were synthesized for biological evaluation. These included 1-amino-1-methyl-2-tetralone and 2-amino-2-methyl-1-tetralone was well as several N-substituted derivatives of these molecules. Locomotor activity testing in mice revealed that 2-amino-2-methyl-1-tetralone caused an increase in locomotor activity while 1-amino-1-methyl-2-tetralone depressed spontaneous locomotor activity. None of the compounds produced hypnosis or profound ataxia.
氯胺酮和苯环己哌啶是结构相似的化合物，具有许多药理作用，其中一些与苯乙胺类的苯丙胺和卡西酮相似。为了整合氯胺酮和卡西酮的结构特征，合成了两组与母体化合物相比构象更受限的类似物，用于生物学评估。这些类似物包括1-氨基-1-甲基-2-四氢萘酮和2-氨基-2-甲基-1-四氢萘酮以及这些分子的几种N-取代衍生物。对小鼠的运动活性测试表明，2-氨基-2-甲基-1-四氢萘酮会导致运动活性增加，而1-氨基-1-甲基-2-四氢萘酮会抑制自发运动活性。这些化合物均未产生催眠作用或严重共济失调。
